SR-4835

For research use only.

Catalog No.S8894

SR-4835 Chemical Structure

Molecular Weight(MW): 499.36

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.

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (200.25 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 499.36
Formula

C21H20Cl2N10O

CAS No. 2387704-62-1
Storage powder
in solvent
Synonyms N/A

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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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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID