An inhibitor of Axl kinase (EC50 = 14 nM); orally bioavailable

R428 – 10 mg

Brand:
Cayman
CAS:
1037624-75-1
Storage:
-20
UN-No:
Non-Hazardous - /

R428 is a small molecule inhibitor of Axl kinase, both in an in vitro biochemical assay and in a cell-based assay using phosphorylation of Ser473 on Akt as the readout (EC50s = 14 nM for both).{33459} It is orally bioavailable, blocks angiogenesis in corneal micropocket and tumor models, and reduces metastatic burden while extending survival in mouse models of breast cancer metastasis.{33459} R428 synergizes with cisplatin (Item No. 13119) to enhance suppression of liver micrometastasis.{33459} R428 is used to study the role of Axl kinase signaling in cancer, cellular senescence, and Zika virus infection.{33458,33460,33461}  

 

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Description

An inhibitor of Axl kinase (EC50 = 14 nM); orally bioavailable, blocks angiogenesis in corneal micropocket and tumor models, and reduces metastatic burden while extending survival in mouse models of breast cancer metastasis

Formal name: 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5Hbenzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine

Synonyms:  ​Bemcentinib|BGB 324

Molecular weight: 506.6

CAS: 1037624-75-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|Zika

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