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Chemical Structure : SR4835
CAS No.: 2387704-62-1
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $358 | In stock | |
| 100 mg | $558 | In stock | |
| 250 mg | Get quote |
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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.
| M.Wt | 499.36 | |
| Formula | C21H20Cl2N10O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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