Abemaciclib | CDK | AmBeed-信号通路专用抑制剂

Abemaciclib {[allProObj[0].p_purity_real_show]}

货号：A106236

Abemaciclib 是一种选择性的 CDK4/6 抑制剂，对 CDK4 和 CDK6 的 IC50 值分别为 2 nM 和 10 nM。Abemaciclib 具有抗肿瘤作用，可用于 HR+/HER2- 乳腺癌和其他肿瘤的研究。

Abemaciclib 化学结构
CAS号：1231929-97-7

Abemaciclib 3D分子结构
CAS号：1231929-97-7

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CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Abemaciclib 生物活性

靶点

CDK4

CDK4, IC50:2 nM
CDK6

CDK6, IC50:10 nM

描述

Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, which also inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib exhibits effectiveness against A375R1-4, M14R, and SH4R cells with EC50 values from 0.3 to 0.6 μM, and similarly inhibits the proliferation of both parental A375 and resistant variants A375RV1 and A375RV2 with IC50 values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib specifically targets CDK4 and CDK6 with low nanomolar potency, leading to G1 arrest and proliferation inhibition in Rb-proficient cells by preventing Rb phosphorylation^[3].

体内研究

In xenograft models, a cooperative antitumor effect is observed when Abemaciclib (45 mg/kg, orally) is combined with RAD001 in HNSCC, and significant tumor growth reduction is noted in A375 xenograft models with doses of 45 or 90 mg/kg^[1]^[2].

体外研究

Abemaciclib exhibits effectiveness against A375R1-4, M14R, and SH4R cells with EC50 values from 0.3 to 0.6 μM, and similarly inhibits the proliferation of both parental A375 and resistant variants A375RV1 and A375RV2 with IC50 values of 395, 260, and 463 nM, respectively^[2].

Abemaciclib specifically targets CDK4 and CDK6 with low nanomolar potency, leading to G1 arrest and proliferation inhibition in Rb-proficient cells by preventing Rb phosphorylation^[3].

作用机制

LY2835219 is a competitive ATP CDK4/6 inhibitor.

Abemaciclib 细胞实验

Cell Line HER2+ breast cancer cell lines TNBC cell lines MDA-MB-231 cells MCF-7 cells MCF7 MDA-MB-453 Human primary fibroblasts (BJ) Human primary fibroblasts (WI38) A549 cells H358 cells PC9 cells MCF7 MCF7AR MCF7 cells MCF7 FAT1-loss cells HCC1428-LTED-AbemaR MCF7-LTED-D538G-AbemaR	Concentration	Treated Time	Description	References
HER2+ breast cancer cell lines	2 µM	24 hours	Evaluate the effect of Sitravatinib combined with CDK4/6 inhibitors on HER2+ breast cancer cells, showing lower sensitivity compared to TNBC cells.	Cancers (Basel). 2024 Jun 18;16(12):2253.
TNBC cell lines	2 µM	24 hours	Evaluate the effect of Sitravatinib combined with CDK4/6 inhibitors on TNBC cells, showing significant suppression of Met, Axl, and MerTK activities.	Cancers (Basel). 2024 Jun 18;16(12):2253.
MDA-MB-231 cells	1 μM	8 days	To assess senescence-like features and sensitivity to lysosomotropic agents in triple-negative breast cancer cells after CDK4/6i treatment. Results showed that abemaciclib-treated MDA-MB-231 cells exhibited senescence-like features and were sensitive to LLOMe and salinomycin.	EMBO J. 2025 Apr;44(7):1921-1942
MCF-7 cells	1 μM	8 days	To assess senescence-like features and sensitivity to lysosomotropic agents in breast cancer cells after CDK4/6i treatment. Results showed that abemaciclib-treated MCF-7 cells exhibited senescence-like features but were insensitive to common senolytic compounds, while being sensitive to lysosomotropic agents LLOMe and salinomycin.	EMBO J. 2025 Apr;44(7):1921-1942
MCF7	500 nM	7 days	To study the effect of Abemaciclib on chromatin accessibility in MCF7 cells, results showed that Abemaciclib induced widespread chromatin remodeling.	Nat Cancer. 2021 Jan;2(1):34-48.
MDA-MB-453	500 nM	7 days	To study the effect of Abemaciclib on chromatin accessibility in MDA-MB-453 cells, results showed that Abemaciclib induced widespread chromatin remodeling.	Nat Cancer. 2021 Jan;2(1):34-48.
Human primary fibroblasts (BJ)	1 µM	8 days	Abemaciclib induced cell cycle arrest, characterized by reduced RB phosphorylation, downregulation of E2F2, and increased p16 expression. Proliferation was not restored after drug withdrawal.	EMBO J. 2022 Mar 15;41(6):e108946.
Human primary fibroblasts (WI38)	1 µM	8 days	Abemaciclib induced cell cycle arrest, characterized by reduced proliferation, and proliferation was not restored after drug withdrawal.	EMBO J. 2022 Mar 15;41(6):e108946.
A549 cells	10 µM	24 h	To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of A549 cells. Results showed that P2shortA significantly inhibited A549 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.	Theranostics. 2020 Jan 12;10(5):2008-2028.
H358 cells	10 µM	24 h	To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of H358 cells. Results showed that P2shortA significantly inhibited H358 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.	Theranostics. 2020 Jan 12;10(5):2008-2028.
PC9 cells	10 µM	24 h	To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of PC9 cells. Results showed that P2shortA significantly inhibited PC9 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.	Theranostics. 2020 Jan 12;10(5):2008-2028.
MCF7	0.1 μM to 20 μM	6 months	To construct MCF7 cells resistant to Abemaciclib and observe the expression changes of PARP1 and p-YB-1. The results showed that with the increase of Abemaciclib concentration, the expression of PARP1 and p-YB-1 was significantly upregulated.	Exp Hematol Oncol. 2023 Nov 30;12(1):100.
MCF7AR	50 μM		To evaluate the resistance of MCF7AR cells to Abemaciclib and verify the expression levels of PARP1 and p-YB-1. The results showed that the IC50 of MCF7AR cells to Abemaciclib was significantly higher than that of MCF7 cells, and the expression of PARP1 and p-YB-1 was upregulated.	Exp Hematol Oncol. 2023 Nov 30;12(1):100.
MCF7 cells	100 nM	24 h	Abemaciclib significantly inhibited the kinase activity of CDK4 but had a weaker effect on CDK6.	Cancer Discov. 2022 Feb;12(2):356-371.
MCF7 FAT1-loss cells	100 nM	24 h	Abemaciclib significantly inhibited the kinase activity of CDK4 but had a weaker effect on CDK6.	Cancer Discov. 2022 Feb;12(2):356-371.
HCC1428-LTED-AbemaR	250 nM	6-12 months	To evaluate the anti-proliferative effect of Abemaciclib in CDK4/6 inhibitor-resistant cells. Results showed that Abemaciclib inhibited the growth of resistant cells in both short-term and long-term proliferation assays, although the extent of inhibition was reduced compared to sensitive cells.	Breast Cancer Res. 2019 Dec 18;21(1):146.
MCF7-LTED-D538G-AbemaR	250 nM	6-10 months	To evaluate the anti-proliferative effect of Abemaciclib in ESR1-mutant CDK4/6 inhibitor-resistant cells. Results showed that Abemaciclib inhibited the growth of resistant cells in both short-term and long-term proliferation assays, although the extent of inhibition was reduced compared to sensitive cells.	Breast Cancer Res. 2019 Dec 18;21(1):146.

Cell Line

Concentration

Treated Time

Description

References

HER2+ breast cancer cell lines

2 µM

24 hours

Evaluate the effect of Sitravatinib combined with CDK4/6 inhibitors on HER2+ breast cancer cells, showing lower sensitivity compared to TNBC cells.

Cancers (Basel). 2024 Jun 18;16(12):2253.

TNBC cell lines

2 µM

24 hours

Evaluate the effect of Sitravatinib combined with CDK4/6 inhibitors on TNBC cells, showing significant suppression of Met, Axl, and MerTK activities.

Cancers (Basel). 2024 Jun 18;16(12):2253.

MDA-MB-231 cells

1 μM

8 days

To assess senescence-like features and sensitivity to lysosomotropic agents in triple-negative breast cancer cells after CDK4/6i treatment. Results showed that abemaciclib-treated MDA-MB-231 cells exhibited senescence-like features and were sensitive to LLOMe and salinomycin.

EMBO J. 2025 Apr;44(7):1921-1942

MCF-7 cells

1 μM

8 days

To assess senescence-like features and sensitivity to lysosomotropic agents in breast cancer cells after CDK4/6i treatment. Results showed that abemaciclib-treated MCF-7 cells exhibited senescence-like features but were insensitive to common senolytic compounds, while being sensitive to lysosomotropic agents LLOMe and salinomycin.

EMBO J. 2025 Apr;44(7):1921-1942

MCF7

500 nM

7 days

To study the effect of Abemaciclib on chromatin accessibility in MCF7 cells, results showed that Abemaciclib induced widespread chromatin remodeling.

Nat Cancer. 2021 Jan;2(1):34-48.

MDA-MB-453

500 nM

7 days

To study the effect of Abemaciclib on chromatin accessibility in MDA-MB-453 cells, results showed that Abemaciclib induced widespread chromatin remodeling.

Nat Cancer. 2021 Jan;2(1):34-48.

Human primary fibroblasts (BJ)

1 µM

8 days

Abemaciclib induced cell cycle arrest, characterized by reduced RB phosphorylation, downregulation of E2F2, and increased p16 expression. Proliferation was not restored after drug withdrawal.

EMBO J. 2022 Mar 15;41(6):e108946.

Human primary fibroblasts (WI38)

1 µM

8 days

Abemaciclib induced cell cycle arrest, characterized by reduced proliferation, and proliferation was not restored after drug withdrawal.

EMBO J. 2022 Mar 15;41(6):e108946.

A549 cells

10 µM

24 h

To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of A549 cells. Results showed that P2shortA significantly inhibited A549 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.

Theranostics. 2020 Jan 12;10(5):2008-2028.

H358 cells

10 µM

24 h

To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of H358 cells. Results showed that P2shortA significantly inhibited H358 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.

Theranostics. 2020 Jan 12;10(5):2008-2028.

PC9 cells

10 µM

24 h

To evaluate the inhibitory effect of Abemaciclib and P2shortA on the proliferation of PC9 cells. Results showed that P2shortA significantly inhibited PC9 cell proliferation at 5-10 µM, and exhibited a synergistic effect when combined with Abemaciclib.

Theranostics. 2020 Jan 12;10(5):2008-2028.

MCF7

0.1 μM to 20 μM

6 months

To construct MCF7 cells resistant to Abemaciclib and observe the expression changes of PARP1 and p-YB-1. The results showed that with the increase of Abemaciclib concentration, the expression of PARP1 and p-YB-1 was significantly upregulated.

Exp Hematol Oncol. 2023 Nov 30;12(1):100.

MCF7AR

50 μM

To evaluate the resistance of MCF7AR cells to Abemaciclib and verify the expression levels of PARP1 and p-YB-1. The results showed that the IC50 of MCF7AR cells to Abemaciclib was significantly higher than that of MCF7 cells, and the expression of PARP1 and p-YB-1 was upregulated.

Exp Hematol Oncol. 2023 Nov 30;12(1):100.

MCF7 cells

100 nM

24 h

Abemaciclib significantly inhibited the kinase activity of CDK4 but had a weaker effect on CDK6.

Cancer Discov. 2022 Feb;12(2):356-371.

MCF7 FAT1-loss cells

100 nM

24 h

Abemaciclib significantly inhibited the kinase activity of CDK4 but had a weaker effect on CDK6.

Cancer Discov. 2022 Feb;12(2):356-371.

HCC1428-LTED-AbemaR

250 nM

6-12 months

To evaluate the anti-proliferative effect of Abemaciclib in CDK4/6 inhibitor-resistant cells. Results showed that Abemaciclib inhibited the growth of resistant cells in both short-term and long-term proliferation assays, although the extent of inhibition was reduced compared to sensitive cells.

Breast Cancer Res. 2019 Dec 18;21(1):146.

MCF7-LTED-D538G-AbemaR

250 nM

6-10 months

To evaluate the anti-proliferative effect of Abemaciclib in ESR1-mutant CDK4/6 inhibitor-resistant cells. Results showed that Abemaciclib inhibited the growth of resistant cells in both short-term and long-term proliferation assays, although the extent of inhibition was reduced compared to sensitive cells.

Breast Cancer Res. 2019 Dec 18;21(1):146.

Abemaciclib 动物实验

Species Nude mice (Foxn1Nu) Mice Mice Mice Mice Mice Nude mice Mice Nude mice	Animal Model MCF-7 tumor model A375 BRAF-mutated melanoma xenografts 786-O cell orthotopic xenografts PDX 14-07 P16-3MR mice H358 orthotopic lung cancer model MDA-MB-231 and MCF7AR xenograft models MCF7 FAT1-loss xenograft model ST941-HI PDX model	Administration	Dosage	Frequency	Description	References
Nude mice (Foxn1Nu)	MCF-7 tumor model	Injection	40 mg/kg	7 consecutive days	To evaluate the inhibitory effect of sequential treatment with CDK4/6i and lysosomotropic agents on breast cancer tumor growth. Results showed that sequential treatment significantly inhibited MCF-7 tumor growth.	EMBO J. 2025 Apr;44(7):1921-1942
Mice	A375 BRAF-mutated melanoma xenografts	Oral	45 mg/kg or 90 mg/kg	Once a day for 56 days	To assess the time course of abemaciclib-mediated target engagement and cell cycle arrest in A375 xenograft tumours, the model successfully described the concentration-dependent time course of pRb, TopoIIa, and pHH3.	Br J Cancer. 2016 Mar 15;114(6):669-79
Mice	786-O cell orthotopic xenografts	Oral gavage	60 mg/kg	Twice daily for 25 days	Abemaciclib suppressed the growth of 786-O xenograft tumors.	Sci Signal. 2019 Oct 1;12(601):eaay0482
Mice	PDX 14-07	Oral	90 mg/kg	Once daily for 21 to 28 days	To study the effect of Abemaciclib on the PDX 14-07 tumor model, results showed that Abemaciclib induced marked gains in H3K27ac.	Nat Cancer. 2021 Jan;2(1):34-48.
Mice	P16-3MR mice	Intraperitoneal injection	50 mg/kg	Once daily for 7 days	Abemaciclib induced p16 expression and SA-β-gal activity in the kidneys of mice, indicating the induction of cellular senescence, but did not cause significant physical performance decline or changes in blood counts.	EMBO J. 2022 Mar 15;41(6):e108946.
Mice	H358 orthotopic lung cancer model	Oral	10 mg/kg	Once daily for three weeks	To evaluate the inhibitory effect of Abemaciclib on the growth of H358 orthotopic lung tumors. Results showed that Abemaciclib alone slightly inhibited tumor growth, while the combination with P2shortA completely inhibited tumor growth.	Theranostics. 2020 Jan 12;10(5):2008-2028.
Nude mice	MDA-MB-231 and MCF7AR xenograft models	Oral and intraperitoneal injection	100 mg/kg	Three times a week	To evaluate the inhibitory effect of combined treatment with Abemaciclib and Olaparib or LJI308 on tumor growth. The results showed that the combined treatment significantly inhibited tumor growth and induced apoptosis of tumor cells.	Exp Hematol Oncol. 2023 Nov 30;12(1):100.
Mice	MCF7 FAT1-loss xenograft model	Intraperitoneal injection	25 mg/kg	3 consecutive days	BSJ-05-017 significantly inhibited the activity of CDK4 and CDK6 and reduced the phosphorylation level of RB1.	Cancer Discov. 2022 Feb;12(2):356-371.
Nude mice	ST941-HI PDX model	Oral	10 mg/kg	Daily for 150 days	To evaluate the anti-tumor activity of Abemaciclib in CDK4/6 inhibitor-resistant PDX models. Results showed that Abemaciclib caused significant tumor growth inhibition in models continuously exposed to Fulvestrant and Palbociclib, indicating that these tumors retain ER-dependent tumor growth despite prior CDK4/6 inhibitor treatment.	Breast Cancer Res. 2019 Dec 18;21(1):146.

Species

Nude mice (Foxn1Nu) Mice Mice Mice Mice Mice Nude mice Mice Nude mice

Animal Model

MCF-7 tumor model A375 BRAF-mutated melanoma xenografts 786-O cell orthotopic xenografts PDX 14-07 P16-3MR mice H358 orthotopic lung cancer model MDA-MB-231 and MCF7AR xenograft models MCF7 FAT1-loss xenograft model ST941-HI PDX model

Administration

Dosage

Frequency

Description

References

Nude mice (Foxn1Nu)

MCF-7 tumor model

Injection

40 mg/kg

7 consecutive days

To evaluate the inhibitory effect of sequential treatment with CDK4/6i and lysosomotropic agents on breast cancer tumor growth. Results showed that sequential treatment significantly inhibited MCF-7 tumor growth.

EMBO J. 2025 Apr;44(7):1921-1942

Mice

A375 BRAF-mutated melanoma xenografts

Oral

45 mg/kg or 90 mg/kg

Once a day for 56 days

To assess the time course of abemaciclib-mediated target engagement and cell cycle arrest in A375 xenograft tumours, the model successfully described the concentration-dependent time course of pRb, TopoIIa, and pHH3.

Br J Cancer. 2016 Mar 15;114(6):669-79

Mice

786-O cell orthotopic xenografts

Oral gavage

60 mg/kg

Twice daily for 25 days

Abemaciclib suppressed the growth of 786-O xenograft tumors.

Sci Signal. 2019 Oct 1;12(601):eaay0482

Mice

PDX 14-07

Oral

90 mg/kg

Once daily for 21 to 28 days

To study the effect of Abemaciclib on the PDX 14-07 tumor model, results showed that Abemaciclib induced marked gains in H3K27ac.

Nat Cancer. 2021 Jan;2(1):34-48.

Mice

P16-3MR mice

Intraperitoneal injection

50 mg/kg

Once daily for 7 days

Abemaciclib induced p16 expression and SA-β-gal activity in the kidneys of mice, indicating the induction of cellular senescence, but did not cause significant physical performance decline or changes in blood counts.

EMBO J. 2022 Mar 15;41(6):e108946.

Mice

H358 orthotopic lung cancer model

Oral

10 mg/kg

Once daily for three weeks

To evaluate the inhibitory effect of Abemaciclib on the growth of H358 orthotopic lung tumors. Results showed that Abemaciclib alone slightly inhibited tumor growth, while the combination with P2shortA completely inhibited tumor growth.

Theranostics. 2020 Jan 12;10(5):2008-2028.

Nude mice

MDA-MB-231 and MCF7AR xenograft models

Oral and intraperitoneal injection

100 mg/kg

Three times a week

To evaluate the inhibitory effect of combined treatment with Abemaciclib and Olaparib or LJI308 on tumor growth. The results showed that the combined treatment significantly inhibited tumor growth and induced apoptosis of tumor cells.

Exp Hematol Oncol. 2023 Nov 30;12(1):100.

Mice

MCF7 FAT1-loss xenograft model

Intraperitoneal injection

25 mg/kg

3 consecutive days

BSJ-05-017 significantly inhibited the activity of CDK4 and CDK6 and reduced the phosphorylation level of RB1.

Cancer Discov. 2022 Feb;12(2):356-371.

Nude mice

ST941-HI PDX model

Oral

10 mg/kg

Daily for 150 days

To evaluate the anti-tumor activity of Abemaciclib in CDK4/6 inhibitor-resistant PDX models. Results showed that Abemaciclib caused significant tumor growth inhibition in models continuously exposed to Fulvestrant and Palbociclib, indicating that these tumors retain ER-dependent tumor growth despite prior CDK4/6 inhibitor treatment.

Breast Cancer Res. 2019 Dec 18;21(1):146.

Abemaciclib 参考文献

Abemaciclib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL

Abemaciclib 技术信息

CAS号	1231929-97-7
分子式	C₂₇H₃₂F₂N₈
分子量	506.59
SMILES Code	CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C
MDL No.	MFCD22665744

别名
运输	蓝冰
InChI Key	UZWDCWONPYILKI-UHFFFAOYSA-N
Pubchem ID	46220502

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 2 mg/mL(3.95 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

Abemaciclib {[allProObj[0].p_purity_real_show]}

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靶点	CDK4 CDK4, IC50:2 nM CDK6 CDK6, IC50:10 nM
描述	Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, which also inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib exhibits effectiveness against A375R1-4, M14R, and SH4R cells with EC50 values from 0.3 to 0.6 μM, and similarly inhibits the proliferation of both parental A375 and resistant variants A375RV1 and A375RV2 with IC50 values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib specifically targets CDK4 and CDK6 with low nanomolar potency, leading to G1 arrest and proliferation inhibition in Rb-proficient cells by preventing Rb phosphorylation^[3].
体内研究	In xenograft models, a cooperative antitumor effect is observed when Abemaciclib (45 mg/kg, orally) is combined with RAD001 in HNSCC, and significant tumor growth reduction is noted in A375 xenograft models with doses of 45 or 90 mg/kg^[1]^[2].
体外研究	Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, which also inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib exhibits effectiveness against A375R1-4, M14R, and SH4R cells with EC50 values from 0.3 to 0.6 μM, and similarly inhibits the proliferation of both parental A375 and resistant variants A375RV1 and A375RV2 with IC50 values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib specifically targets CDK4 and CDK6 with low nanomolar potency, leading to G1 arrest and proliferation inhibition in Rb-proficient cells by preventing Rb phosphorylation^[3].
作用机制	LY2835219 is a competitive ATP CDK4/6 inhibitor.

Abemaciclib {[allProObj[0].p_purity_real_show]}

Abemaciclib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Abemaciclib 质控信息

Abemaciclib 生物活性

Abemaciclib 细胞实验

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Abemaciclib 参考文献

Abemaciclib 实验方案

Abemaciclib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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