PHA-793887 | CDK Inhibitor | AmBeed-信号通路专用抑制剂

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PHA-793887 {[allProObj[0].p_purity_real_show]}

货号：A184364

PHA-793887是一种 CDK 抑制剂，能够抑制 CDK1、CDK2、CDK4 和 CDK9 的活性，IC50 分别为 8 nM、60 nM、62 nM 和 138 nM，具有抗癌活性并可诱导细胞周期停滞和凋亡。

PHA-793887 化学结构
CAS号：718630-59-2

PHA-793887 3D分子结构
CAS号：718630-59-2

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PHA-793887 纯度/质量文件产品仅供科研

货号：A184364 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

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											ERK,SGK	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/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 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/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 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/CyclinE, IC50: 8 nM CDK2/CyclinA, 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/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 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/CyclinE, IC50: 0.7 μM CDK2/CyclinA, 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ 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												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 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。

PHA-793887 生物活性

靶点	CDK5 CDK5/p25, IC50:5 nM CDK4 CDK4/CyclinD1, IC50:62 nM CDK2 CDK2/CyclinE, IC50:8 nM CDK2/CyclinA, IC50:8 nM CDK9 CDK9/CyclinT1, IC50:138 nM
描述	Cyclin dependent kinases (CDKs) are a family of serine/threonine kinases that, in concert with cyclins (positive regulators) and natural inhibitors (CDKI), control the cell cycle progression. PHA -793887 is a novel and effective CDK2, CDK5 and CDK7 inhibitor with IC₅₀ of 8 nM, 5 nM and 10 nM, respectively. A2780 ovarian carcinoma cells were treated with PHA-793887 for 24 h at the concentration of 3 μM and 1 μM. A decrease in the S phase population and a subsequent increase of the G1 population, as expected for inhibition of CDK2/cyclin A, were observed at 1 μM treatment compared to the control cells. At 3 μM only a strong G2/M increase was observed, which can be ascribed to inhibition of CDK1/cyclin B. The presence of cells with sub G1 DNA content (from 2.6% in control cells to 26.2% in cells treated with PHA-793887 at 3 μM) clearly implied cell death and apoptosis. A clear reduction in DNA synthesis was observed, compared to the control group. A clear reduction of the hyperphosphorylated form of pRb (retinoblastoma protein, a known CDK substrate) and an accumulation of the hypophosphorylated form of pRb were observed in the extracts of treated cell. PHA-793887 (1 or 3 μM) decreases the amount of pRB (retinoblastoma protein, a known CDK substrate) phosphorylation in treated cells in comparison with untreated cells. PHA-793887 caused a dose-dependent inhibition of the A2780 tumor growth up to 76% at the dose of 30 mg/kg in the human ovarian A2780 xenograft mouse model^[4].
作用机制	The pyrrolo-pyrazole system of PHA-793887 occupies the adenine region of the ATP pocket, while the iso-butyl group points towards the solvent accessible region.

PHA-793887 细胞实验

Cell Line A549 cells U2OS cells Ishikawa cells HEC-1B cells KLE cells	Concentration	Treated Time	Description	References
A549 cells	0.5 µM		PHA793887 inhibited the upregulation of TREM2, BLNK, STING1, and CASP1, and induced the activation of caspase-3	Int J Mol Sci. 2021 Oct 14;22(20):11072.
U2OS cells	10 µM	16 h	To evaluate the inhibitory effect of PHA-793887 on CDK5-p25 protein-protein interaction, results showed that PHA-793887 significantly reduced the number of BiFC positive cells	Sci Rep. 2018 Mar 23;8(1):5083.
Ishikawa cells	10^-6 M	48 h	Evaluate the effect of PHA-793887 on Ishikawa cells, results showed that PHA-793887 significantly increased caspase 3/7 activity (p < 0.05).	Sci Rep. 2023 Aug 23;13(1):13763.
HEC-1B cells	10^-6 M	48 h	Evaluate the effect of PHA-793887 on HEC-1B cells, results showed that PHA-793887 significantly decreased caspase 3/7 activity (p < 0.05).	Sci Rep. 2023 Aug 23;13(1):13763.
KLE cells	10^-6 M	48 h	Evaluate the effect of PHA-793887 on KLE cells, results showed that PHA-793887 significantly reduced glucose consumption (p < 0.05).	Sci Rep. 2023 Aug 23;13(1):13763.

PHA-793887 动物研究

Dose

CD-1 nude mice: 15 mg/kg, 30 mg/kg^[3] (i.v.)

Administration

i.v.

Pharmacokinetics

Animal	Nude mice^[1]
Dose	10 mg/kg
Administration	i.v.
T_1/2	4.1 h
AUC	19.2 μM·h
CL	23.9 ml/min/kg
C_max	36.5 μM
V_ss	1360 ml/kg

PHA-793887 参考文献

[1]Brasca MG, Albanese C, et al. Optimization of 6,6-dimethyl pyrrolo[3,4-c] pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53.

[2]Alzani R, Pedrini O, et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp Hematol. 2010 Apr;38(4):259-269.e2.

[3]Locatelli G, Bosotti R, et al. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May;9(5):1265-73.

[4]Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M. Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25. PMID: 20153204.

PHA-793887 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.66mL

5.53mL

2.77mL

PHA-793887 技术信息

CAS号	718630-59-2
分子式	C₁₉H₃₁N₅O₂
分子量	361.48
SMILES Code	CC(C)CC(NC1=NNC2=C1CN(C(C3CCN(C)CC3)=O)C2(C)C)=O
MDL No.	MFCD17169992

别名
运输	蓝冰
InChI Key	HUXYBQXJVXOMKX-UHFFFAOYSA-N
Pubchem ID	46191454

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(138.32 mM)，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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；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

human A2780 cells		Proliferation assay	72 h	Antiproliferative activity against human A2780 cells after 72 hrs by fluorescence assay, IC50=0.09 μM	20153204
human A2780 cells	3 μM	Function assay		Inhibition of CDK in human A2780 cells assessed as accumulation of hypophosphorylated form of retinoblastoma protein at 3 uM by immunohistochemistry	20153204
human A375 cells		Proliferation assay	72 h	Antiproliferative activity against human A375 cells after 72 hrs by SRB assay, IC50=0.396 μM	20153204
human BxPC3 cells		Proliferation assay	72 h	Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB assay, IC50=3.444 μM	20153204
human C-433 cells		Proliferation assay	72 h	Antiproliferative activity against human C-433 cells after 72 hrs by SRB assay, IC50=0.285 μM	20153204
human COLO205 cells		Proliferation assay	72 h	Antiproliferative activity against human COLO205 cells after 72 hrs by SRB assay, IC50=0.188 μM	20153204
human DU145 cells		Proliferation assay	72 h	Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay, IC50=0.303 μM	20153204
human HCT116 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.163 μM	20153204
human MCF7 cells		Proliferation assay	72 h	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay, IC50=1.284 μM	20153204
human PC3 cells		Proliferation assay	72 h	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.601 μM	20153204

PHA-793887 {[allProObj[0].p_purity_real_show]}

PHA-793887 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PHA-793887 质控信息

PHA-793887 生物活性

PHA-793887 细胞实验

PHA-793887 动物研究

PHA-793887 参考文献

PHA-793887 实验方案

PHA-793887 技术信息

最近浏览的产品

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靶点

总药量计算器

工作液计算器

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临床研究

确认信息

热门区域

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CDK5	CDK5/p25, IC50:5 nM
CDK4	CDK4/CyclinD1, IC50:62 nM
CDK2	CDK2/CyclinE, IC50:8 nM CDK2/CyclinA, IC50:8 nM
CDK9	CDK9/CyclinT1, IC50:138 nM
CDK7	CDK7/CyclinH, IC50:10 nM
CDK1	CDK1/CyclinB, IC50:60 nM

PHA-793887 {[allProObj[0].p_purity_real_show]}

PHA-793887 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PHA-793887 质控信息

PHA-793887 生物活性

PHA-793887 细胞实验

PHA-793887 动物研究

PHA-793887 参考文献

PHA-793887 实验方案

PHA-793887 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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PHA-793887 纯度/质量文件产品仅供科研