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R 428 dihydrochloride
- BGB324 - Bemcentinib
Axon 1946
- Parent CAS: 1037624-75-1
- Optical Purity: 99% e.e.
- Soluble in water and DMSO
- MF: C30H34N8.2HCl
- MW: 579.57
Description
R 428 dihydrochloride (Bemcentinib) is a potent and selective Axl receptor tyrosine kinase inhibitor with reported IC50 activity of 14 nM. It inhibits Axl kinase activation and blocks downstream events including Akt phosphorylation, cell invasion and inflammatory cytokine production.
The Gas6-Axl axis contributes to epithelial-to-mesenchymal transition, tumor cell survival, metastasis, immune evasion and therapy resistance. R 428 is used to investigate Axl-dependent signaling in oncology, inflammation and immune-oncology models.
Key Features
- Potent Axl receptor tyrosine kinase inhibitor
- Reported IC50: 14 nM
- Blocks Gas6-Axl signaling and downstream Akt activation
- Relevant to invasion, metastasis and immune modulation research
Applications
- Axl kinase signaling studies
- Cancer invasion and EMT models
- Immune-oncology pathway research
- RTK inhibitor profiling
More Information
| Parent CAS No. | 1037624-75-1 |
|---|---|
| Chemical Name | 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]- dihydrochloride |
| SMILES | N1(C2=NN=C3C4=CC=CC=C4CCCC3=C2)C(N)=NC(NC2=CC=C3CC[C@H](N4CCCC4)CCC3=C2)=N1.Cl.Cl |&1:27,r| |
| MFCD | N.A. |
| 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/t25-;;/m0../s1 |
| InChiKey | KNUMGBTVVFIGFU-WLOLSGMKSA-N |
| CID | 91826491 |
| Short Description | Axl inhibitor |
References
- 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.
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