A Cdk12 and Cdk13 inhibitor
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SR 4835

Item No. 39158

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(5,6-dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methyl-1H-pyrazol-4-yl)-2-(4-morpholinyl)-9H-purin-6-amine
CAS Number
2387704-62-1
Molecular Formula
C21H20Cl2N10O
Formula Weight
499.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
λmax
212, 293, 299 nm
SMILES
ClC1=CC2=C(C=C1Cl)NC(CNC3=NC(N4CCOCC4)=NC5=C3N=CN5C6=CN(C)N=C6)=N2
InChi Code
InChI=1S/C21H20Cl2N10O/c1-31-10-12(8-26-31)33-11-25-18-19(29-21(30-20(18)33)32-2-4-34-5-3-32)24-9-17-27-15-6-13(22)14(23)7-16(15)28-17/h6-8,10-11H,2-5,9H2,1H3,(H,27,28)(H,24,29,30)
InChi Key
FSELUFUYNUNZKD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $40

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    10 mg

    $64

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    25 mg

    $139

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    50 mg

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    Product Description

    SR 4835 is an inhibitor of cyclin-dependent kinase 12 (Cdk12) and Cdk13.1 It binds to Cdk12 and Cdk13 (Kds = 98 and 4.9 nM, respectively) and inhibits Cdk12- and Cdk13-dependent phosphorylation of RNA polymerase II in MDA-MB-231 cells (EC50 = 105.5 nM). SR 4835 inhibits the proliferation of MDA-MB-231, MDA-MB-468, Hs 578T, and MDA-MB-436 breast cancer cells (EC50s = 15.5, 22.1, 19.9, and 24.9 nM, respectively). It induces the DNA damage response and apoptosis in MDA-MB-231 cells when used at concentrations ranging from 30 to 90 nM. In vivo, SR 4835 (20 mg/kg) reduces tumor volume and decreases the number of mice with tumors greater than 1,000 mm3 in a patient-derived xenograft (PDX) model of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Quereda, V., Bayle, S., Vena, F., et al. Therapeutic targeting of CDK12/CDK13 in triple-negative breast cancer. Cancer Cell 36(5), 545-558 (2019).