A dual inhibitor of FLT3 and Cdk4 (IC50s = 1 and 3 nM

AMG 925 – 25 mg

Brand:
Cayman
CAS:
1401033-86-0
Storage:
-20
UN-No:
Non-Hazardous - /

AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4; IC50s = 1 and 3 nM, respectively).{48702} It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.  

 

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SKU: 29245 - 25 mg Category:

Description

A dual inhibitor of FLT3 and Cdk4 (IC50s = 1 and 3 nM, respectively); selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 μM); also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM); inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively); reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 AML mouse xenograft model

Formal name: 1-[7,8-dihydro-2-[[9-(trans-4-methylcyclohexyl)-9H-pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,6-naphthyridin-6(5H)-yl]-2-hydroxy-ethanone

Synonyms: 

Molecular weight: 471.6

CAS: 1401033-86-0

Purity: ≥95%

Formulation: A crystalline solid

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