For research use only. Not for therapeutic Use.
Potent and selective inhibitor of Axl receptor tyrosine kinases (IC50: 14 nM); R428 inhibits Axl kinase and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.
Note: The hydrochloride salt of R428 is water-soluble and has an improved solubility in DMSO in comparison with its free base
KEYWORDS: R 428 dihydrochloride | supplier | Axl inhibitor | BGB324 | R428 HCl | R-428 | BGB-324 | CAS [2108833-51-6] | [1037624-75-1] | Gas6 | Axl | receptor tyrosine kinase | RTK | Akt | breast cancer | proinflammatory | cytokine production
| Catalog Number | I047579 |
| CAS Number | 2108833-51-6 |
| Molecular Formula | C30H34N8.2HCl |
| Purity | ≥95% |
| IUPAC Name | 1-(3,4-diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-yl)-3-N-(7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl)-1,2,4-triazole-3,5-diamine;dihydrochloride |
| InChI | InChI=1S/C30H34N8.2ClH/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27;;/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36);2*1H |
| SMILES | C1CCN(C1)C2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76.Cl.Cl |
| Reference | SJ Holland et al. R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer. Cancer Res. 2010, 70, 1544.
Ghosh AK et al. The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy. Blood, 2011, 117(6), 1928-37.
GX Ruan and A Kazlauskas. Axl is essential for VEGF-A-dependent activation of PI3K/Akt. EMBO J. 2012, 31(7), 1692-1703. |
