SR-4835

Catalog No.S8894

For research use only.

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.

SR-4835 Chemical Structure

CAS No. 2387704-62-1

Purity & Quality Control

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Biological Activity

Description SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.
Targets
CDK13 [1]
(Cell-free assay)
CDK12 [1]
(Cell-free assay)
CDK12 [1]
(Cell-free assay)
4.9 nM 98 nM(Kd) 99 nM
In vitro

SR-4835 is a selective, potent dual inhibitor of CDK12 and CDK13, suppressing expression of DDR proteins. CDK12/CDK13 inhibition synergizes with DNA-damaging agents or PARP inhibition to trigger TNBC cell death.[1]

In vivo

SR-4835 has potent in vivo anti-TNBC activity and augments the anti-cancer activity of cisplatin, irinotecan, and olaparib, which are standard-of-care therapeutics for TNBC. SR-4835 is well tolerated in mice after long-term dosing. SR-4835 cooperates with DNA-damaging chemotherapeutics.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Human: MDA-MB-231, MDA-MB-436, HS578T, MDA-MB-468, FHC
  • Concentrations: 10-90 nM, 0.4-10 μM
  • Incubation Time: 4 h, 6 h, 72 h
  • Method:

    Clonogenic Assays. 500 cells per well are plated in six-well dishes in triplicate. After overnight incubation, SR-4835 is added to the medium for 72 hr, and cells are allowed to grow for 7 to 10 days, during which medium is changed every 2 to 3 days.

Animal Research:

[1]

  • Animal Models: Female SCID Beige mice bearing xenograft tumor fragments, male C57Bl-6 mice
  • Dosages: 20 mg/kg
  • Administration: Oral gavage, IV

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 499.36
Formula

C21H20Cl2N10O

CAS No. 2387704-62-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)N2C=NC3=C(N=C(N=C32)N4CCOCC4)NCC5=NC6=CC(=C(C=C6N5)Cl)Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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