A potent inhibitor of Aurora kinases (IC50s = 15

CCT137690 – 50 mg

Brand:
Cayman
CAS:
1095382-05-0
Storage:
-20
UN-No:
Non-Hazardous - /

CCT137690 is a potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively).{27919} It also inhibits the receptor tyrosine kinase FLT3 as well as the constitutively active form of FLT3 bearing internal-tandem duplications (FLT3-ITD; IC50s = 1.2 and 4.9 nM, respectively).{27919} CCT137690 is orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice without inducing body weight loss.{27919} It blocks signaling through Aurora kinases in MYCN-amplified neuroblastoma cells, suppressing N-Myc expression and preventing proliferation.{27916} It inhibits growth of FLT3-ITD cells harboring a D835Y mutation, which confers resistance to other FLT3 inhibitors.{27917} CCT137690 also sensitizes colorectal carcinoma cells to radiotherapy.{27918}  

 

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Description

A potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively); also inhibits FLT3 as well as the constitutively active FLT3-ITD form (IC50s = 1.2 and 4.9 nM, respectively); orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice

Formal name: 6-bromo-7-[4-[(5-methyl-3-isoxazolyl)methyl]-1-piperazinyl]-2-[4-(4-methyl-1-piperazinyl)phenyl]-3H-imidazo[4,5-b]pyridine

Synonyms: 

Molecular weight: 551.5

CAS: 1095382-05-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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