An inhibitor of Src family kinases

A-419259 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1435934-25-0
Storage:
-20
UN-No:
Non-Hazardous - /

A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}  

 

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Description

An inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM); inhibits growth of Ph­+ K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells; induces apoptosis in K-562 cells in a concentration-dependent manner; inhibits differentiation of murine embryonic stem cells while maintaining pluripotency at 300 nM; reduces the total number of AML cells, as well as AML stem cells, in the bone marrow and spleen of human patient-derived AML mouse xenograft models at 30 mg/kg twice daily

Formal name: 7-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, trihydrochloride

Synonyms:  RK-20449

Molecular weight: 592

CAS: 1435934-25-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|SRC Family Signaling||Research Area|Cell Biology|Stem Cell Research|Differentiation

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