2387704-74-5
Chemical Structure
SR-5037
- CAS No.: 2387704-74-5
- Formula:C21H18Cl2F2N10O
- Molecular Weight:535.34
InChIKey: CUNVHFMIKBBAIC-UHFFFAOYSA-N
SMILES: ClC1=C(C=C(N2)C(N=C2CNC3=C4C(N(C=N4)C(C=N5)=CN5C(F)F)=NC(N6CCOCC6)=N3)=C1)Cl
Biological Activity: SR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer[1].
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SR-5037 | 99.58% | SR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer. | ||||||||||||||||||||
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Keywords