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SR-4835

Chemical Structure : SR-4835

CAS No.: 2387704-62-1

SR-4835 (SR4835, SR 4835)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 499.36
Formula C21H20Cl2N10O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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