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Chemical Structure : R428
CAS No.: 1037624-75-1
Catalog No.: PC-20336Not For Human Use, Lab Use Only.
R428 (Bemcentinib, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | Get quote |
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R428 (Bemcentinib, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM.
R428 inhibits phosphorylation of Akt (Ser473) and Axl (Tyr821) in cell-based activity assays.
R428 exhibits>100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells.
R428 is >100-fold selective for Axl over insulin receptor,EGFR, HER2, and PDGFRβ and kinases of other subfamilies.
R428 (0-3 uM) dose dependently suppresses invasion of both human MDA-MB-231 and murine 4T1 breast cancer cell lines.
R428 (125 mg/kg, BID) suppresses breast cancer metastasis in MDA-MB-231 xenograft and orthotopic 4T1 models.
R428 suppresses angiogenesis in vivo and modulates expression of surrogate markers in tumor tissue.
| M.Wt | 506.66 | |
| Formula | C30H34N8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-((7-pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine |
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1. Holland SJ, et al. Cancer Res. 2010 Feb 15;70(4):1544-54.
2. Hector A, et al. Cancer Biol Ther. 2010 Nov 15;10(10):1009-18.
3. Lijnen HR, et al. J Pharmacol Exp Ther. 2011 May;337(2):457-64.
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