SR-4835

Catalog No.S8894 Batch:S889401

Technical Data

Formula	C₂₁H₂₀Cl₂N₁₀O
Molecular Weight	499.36	CAS No.	2387704-62-1
Solubility (25°C)*	In vitro	DMSO	60 mg/mL (120.15 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. 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

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

References

[1] Quereda V, et al. Cancer Cell. 2019 Nov 11;36(5):545-558.e7.

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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.

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