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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-SR4835
SR4835

Chemical Structure : SR4835

CAS No.: 2387704-62-1

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SR4835 (SR-4835, SR 4835)

货号: PC-73102Not For Human Use, Lab Use Only.

SR-4835 (SR4835) is a potent, highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 98 and 4.9 nM, respectively.

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10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg ￥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SR-4835 (SR4835) is a potent, highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 98 and 4.9 nM, respectively.
SR-4835 is highly selective toward CDK12 and CDK13 when tested in a panel of over 450 kinases at 10 uM, including CDK4, CDK6, CDK9, GSK3A, and GSK3B.
SR-4835 blocks Ser2 phosphorylation on the CTD of RNA Pol II (EC50=100 nM), has no affinity to BRD4 and does not inhibit PARP activity.
SR-4835 blocked clonogenic growth and survival of MDA-MB-231 cells (IC50=15.5 nM) with increased potency over THZ531.
SR-4835 suppressed the expression of DNA damage repair proteins accompanied with increased DNA damage and cell death in tumor cells.
SR-4835 synergizes with DNA-damaging chemotherapeutics cisplatin and provokes TNBC cell death by downregulating DNA repair proteins.
SR-4835/Cisplatin combination provokes tumor regression in an orthotopic TNBC PDX model.
SR-4835/Irinotecan combination provokes regression in BRCA1-deficient PDX model.

物理化学性质&存储条件

分子量 499.36
分子式 C21H20Cl2N10O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((5,6-dichloro-1H-benzo[d]imidazol-2-yl)methyl)-9-(1-methyl-1H-pyrazol-4-yl)-2-morpholino-9H-purin-6-amine

参考文献

1. Quereda V, et al. Cancer Cell. 2019 Nov 11;36(5):545-558.e7.

2. Hopkins JL, et al. Cancer Cell. 2019 Nov 11;36(5):461-463.

3. Li Y, et al. Cancer Lett. 2020 Dec 28;495:12-21.

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