SR-4835

Catalog No.S8894 Batch:S889402

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Technical Data

Formula

C21H20Cl2N10O
Molecular Weight 499.36 CAS No. 2387704-62-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (200.25 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 olaparib, which is 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 Assay:

[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 Study:

[1]
  • Animal Models

    Female SCID Beige mice bearing xenograft tumor fragments, male C57Bl-6 mice

  • Dosages

    20 mg/kg

  • Administration

    Oral gavage, IV

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.