An inhibitor of Aurora A

PHA-680632 – 5 mg

Brand:
Cayman
CAS:
398493-79-3
Storage:
-20
UN-No:
Non-Hazardous - /

PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively).{48527} It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.  

 

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Description

An inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively); has >15-fold selectivity for Aurora A kinase in a panel of 31 kinases; inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM); inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cancer cell lines (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively); reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia xenograft mouse model when administered at a dose of 45 mg/kg

Formal name: N-(2,6-diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]-pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide

Synonyms: 

Molecular weight: 501.6

CAS: 398493-79-3

Purity: ≥98%

Formulation: A crystalline solid

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