AZD-5438 | CDK | AmBeed-信号通路专用抑制剂

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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。

靶点	CDK2 CDK2, IC50:6 nM CDK9 CDK9, IC50:20 nM CDK1 CDK1, IC50:16 nM
描述	The regulatory proteins that control cell cycle progression are the cyclins, cyclin-dependent kinases (cdks). Cdk inhibitors preferentially target proliferating cells and induce cell death, thus making cdks among the most highly attractive targets for therapeutic intervention in cancer. AZD5438 is a potent inhibitor of cdk 1, 2, and 9 with IC₅₀ values of 16, 6, and 20 nM, respectively. In vitro, AZD5438 showed significant antiproliferative activity in human tumor cell lines with an IC₅₀ value ranging from 0.2 to 1.7 μM, causing inhibition of the phosphorylation of cdk substrates pRb, nucleolin, protein phosphatase 1a, and RNA polymerase II COOH-terminal domain and blocking cell cycling at G₂-M, S, and G₁ phases. In vivo, when orally administered at either 50 mg/kg twice daily or 75 mg/kg once daily, AZD5438 inhibited human tumor xenograft growth (maximum percentage tumor growth inhibition, range, 38-153; P < 0.05)^[3]. In human xenograft animal models using athymic nude mice, combined treatment with AZD5438 and irradiation enhanced tumor growth delay, with an enhancement factor ranging from 1.2-1.7^[4].
作用机制	There is a hydrogen-bonding interaction between imidazole of AZD5438 and the hinge region of cdks^[3].

Cell Line Zebrafish larvae HEI-OC1 cells Mouse cochlear explants P3 mouse cochlear explants A549 H1299 H460 PANC-1 cells Human naive pluripotent stem cells Caco2 cells IEC-6 cells HEK 293T cells	Concentration	Treated Time	Description	References
Zebrafish larvae	50 nM	2 hours	To test the synergistic protective effect of AZD-5438 with zorifertinib, results showed that AZD-5438 and zorifertinib at 50 nM concentration had a synergistic protective effect on excitotoxic damage in zebrafish larvae.	Sci Adv. 2024 Jun 21;10(25):eadk2299.
HEI-OC1 cells	0.700 µM	22 hours	To evaluate the protective effect of AZD-5438 against cisplatin-induced cytotoxicity, the results showed an EC50 of 0.700 μM in HEI-OC1 cells.	J Med Chem. 2018 Sep 13;61(17):7700-7709.
Mouse cochlear explants	0.34 nM	24 hours	To test the protective effect of AZD5438 against cisplatin-induced hair cell death in cochlear explants, results showed that AZD5438 combined with dabrafenib provided enhanced protection compared to each drug alone.	Sci Adv. 2020 Dec 2;6(49):eabd0561.
P3 mouse cochlear explants	0.005 µM	24 hours	To evaluate the protective effect of AZD-5438 against cisplatin-induced toxicity in cochlear explants, the results showed an EC50 of 0.005 μM in explants.	J Med Chem. 2018 Sep 13;61(17):7700-7709.
A549	75 nM	24 hours	AZD5438 significantly enhanced the radiosensitivity of A549 cells, with a dose enhancement ratio (DER) of 1.5.	Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14.
H1299	50 nM	24 hours	AZD5438 significantly enhanced the radiosensitivity of H1299 cells, with a dose enhancement ratio (DER) of 1.3.	Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14.
H460	200 nM	24 hours	AZD5438 significantly enhanced the radiosensitivity of H460 cells, with a dose enhancement ratio (DER) of 1.3.	Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14.
PANC-1 cells	0.5 µM, 0.1 µM, 0.02 µM	3 weeks	AZD-5438 significantly inhibited the clonogenic capacity of PANC-1 cells, indicating its ability to suppress PDAC cell proliferation by activating C/EBPδ.	J Cell Mol Med. 2025 Feb;29(3):e70287.
Human naive pluripotent stem cells	0.1 µM	4-5 days	AZD5438 was able to maintain the naive state of human naive pluripotent stem cells in feeder-free conditions and prevent exit from pluripotency.	Stem Cell Reports. 2019 Oct 8;13(4):612-626.
Caco2 cells	5 µM	48 hours	AZD5438 completely blocked the growth of Caco2 cells and induced apoptosis.	Apoptosis. 2014 Mar;19(3):451-66.
IEC-6 cells	1 µM	72 hours	AZD5438 significantly reduced proliferation of IEC-6 cells and induced apoptosis.	Apoptosis. 2014 Mar;19(3):451-66.
HEK 293T cells	1 µM	72 hours	AZD-5438, as a CDK inhibitor, significantly induced C/EBPδ-mediated eGFP fluorescence, indicating its ability to activate C/EBPδ transcriptional activity.	J Cell Mol Med. 2025 Feb;29(3):e70287.

Species Mice BALB/c Nude mice Nude mice Mice Zebrafish FVB mice	Animal Model NOD/SCID mice AFPGC PDX models Human xenograft model Noise-induced hearing loss model Excitotoxicity model Cisplatin-induced ototoxicity model	Administration	Dosage	Frequency	Description	References
Mice	NOD/SCID mice	Oral	20 mg/kg	Once daily for three weeks	To evaluate the antitumor activity of AZD-5438 in PDX models with high CCNE1 copy number. AZD-5438 showed significant antitumor activity in models with high CCNE1 copy number by inhibiting the expression of CDK2, CCNE1, and phosphorylated Rb.	J Hematol Oncol. 2018 Feb 13;11(1):20
BALB/c Nude mice	AFPGC PDX models	Oral	20 mg/kg	Daily for 3 weeks	To evaluate the antitumor efficacy of AZD5438 in CCNE1-amplified AFPGC PDX models, the results showed that AZD5438 significantly inhibited tumor growth in CCNE1-amplified models.	Nat Commun. 2021 Jun 24;12(1):3946
Nude mice	Human xenograft model	Oral	25 mg/kg/day	Once daily for 5 days	Combined treatment with AZD5438 and irradiation significantly enhanced tumor growth delay, with A549 and H1299 xenografts showing good response to the combined treatment.	Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14.
Mice	Noise-induced hearing loss model	Oral	35 mg/kg	Twice daily for 24, 48, and 72 hours	To test the protective effect of AZD5438 against noise-induced hearing loss, results showed that AZD5438 combined with dabrafenib provided significant hearing protection.	Sci Adv. 2020 Dec 2;6(49):eabd0561.
Zebrafish	Excitotoxicity model	In vitro culture	50 nM	Single dose, 2 hours	To test the synergistic protective effect of AZD-5438 with zorifertinib, results showed that AZD-5438 and zorifertinib at 50 nM concentration had a synergistic protective effect on excitotoxic damage in zebrafish larvae.	Sci Adv. 2024 Jun 21;10(25):eadk2299.
FVB mice	Cisplatin-induced ototoxicity model	Transtympanic injection	50 μM	1 hour before cisplatin administration and again 24 hours after cisplatin administration	To evaluate the protective effect of AZD-5438 against cisplatin-induced ototoxicity, the results showed that AZD-5438 significantly reduced ABR threshold shifts at 32 kHz, providing complete protection.	J Med Chem. 2018 Sep 13;61(17):7700-7709.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00088790	Neoplasms	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Research Site Boston, Massachusetts, United States United States, New York Research Site New York City, New York, United States 收起 <<

CAS号	602306-29-6
分子式	C₁₈H₂₁N₅O₂S
分子量	371.46
SMILES Code	O=S(C1=CC=C(NC2=NC=CC(C3=CN=C(C)N3C(C)C)=N2)C=C1)(C)=O
MDL No.	MFCD11112135

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别名
运输	蓝冰
InChI Key	WJRRGYBTGDJBFX-UHFFFAOYSA-N
Pubchem ID	16747683

human LoVo cells		Proliferation assay	48 h	Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs, IC50=0.63 μM	18815031
human LoVo cells		Proliferation assay	48 h	Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs, IC50=0.8 μM	18996007

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