R428 (BGB324), AXL inhibitor

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MW 506.6 Da, Purity >98%. Potent and selective inhibitor of AXL kinase (IC₅₀ = 14 nM). Overcomes chemotherapy resistance to various agents in multiple cancer models. Suppresses myeloid cell activation and function. AXL inhibition combined with PD-1 blockade shows potent synergistic anti-tumor effects. Greater than 100-fold selective for AXL versus ABL. Selective (50-100-fold) versus Mer and Tyro3 in cell-based assays. Highly selective for AXL versus InsR, EGFR, HER2, and PDGFRbeta in cell-free assays.

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AI323647, AIK, AIK2, ALK tyrosine kinase receptor, ALK/EML4 fusion gene, included, ALK/NPM1 fusion gene, included, ALK_HUMAN, ARK-1, ARK-2, ASV, AURA, AURKB_HUMAN, AURORA/IPL1-like kinase, AUTS9, AW259666, AXL oncogene, AXL receptor tyrosine kinase, AXL transforming gene, AXL transforming sequence/gene, Adhesion related kinase, Alpha-type platelet-derived growth factor receptor, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase Ki1, Ark, AurB, Aurora 1, Aurora 2, Aurora A, Aurora kinase A, Aurora kinase B, Aurora- and Ipl1-like midbody-associated protein 1, Aurora-B, Aurora-related kinase 1, Aurora-related kinase 2, Aurora/IPL1-related kinase 1, Aurora/IPL1-related kinase 2, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, Avian sarcoma virus, BTAK, BYK, Breast tumor-amplified kinase, Brt, C SRC, CAK, CD 135, CD 167, CD 246, CD135 antigen, CD140 antigen-like family member A, CD140A, CD140a antigen, CD167 antigen-like family member A, CD167a, CD246 antigen, CD309, CD309 antigen, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, Cell adhesion kinase, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, D249, DDR, DDR1_HUMAN, DTK, Discoidin domain receptor, Discoidin domain receptor tyrosine kinase 1, Discoidin receptor tyrosine kinase, Discoidin receptor tyrosine kinase isoform a, EC 2.7.10.1, EC 2.7.10.2, EDDR 1, EGFR_HUMAN, ERBB, ERBB1, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Epithelial discoidin domain receptor 1, Epithelial discoidin domain-containing receptor 1, Epithelial specific receptor kinase, Errp, Etk-2, Eyk, FL cytokine receptor, FLK-1, FLK1, mouse, homolog of, FLT3_HUMAN, Fetal liver kinase 1, Fetal liver kinase 2, Flk 2, Fms related tyrosine kinase 3, Fms-like tyrosine kinase 3, Growth factor receptor tyrosine kinase type III, HER1, HGF receptor, HGF/SF receptor, HGFR, HGK2, Hepatocyte growth factor receptor, IAK, IPL1, IPL1 related kinase, JTK11, KI 1, KRD1, Kdr, Kinase insert domain receptor, Kinase insert domain receptor (a type III receptor tyrosine kinase), Ly-72, Ly73, MCK-10, MER, MER receptor tyrosine kinase, MERK, MERPEN, MERTK c-mer proto-oncogene tyrosine kinase, MERTK_HUMAN, MET proto oncogene, receptor tyrosine kinase, MET_HUMAN, MGC133349, MGC34538, MGC74795, Mammarian carcinoma kinase 10, Mammary carcinoma kinase 10, Met proto oncogene tyrosine kinase, Met proto-oncogene, Met proto-oncogene (hepatocyte growth factor receptor), NBLST 3, NISBD2, NTRK 4, Neuroepithelial tyrosine kinase, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, Neurotrophic tyrosine kinase receptor type 4, Nyk, OTTHUMP00000029343, OTTHUMP00000029344, OTTHUMP00000029345, OTTHUMP00000029346, OTTHUMP00000029347, OTTHUMP00000031340, OTTHUMP00000031341, OTTHUMP00000031342, OTTHUMP00000031343, OTTHUMP00000031344, OTTHUMP00000031345, OTTHUMP0000004234, OTTHUMP00000164863, OTTHUMP00000164867, OTTHUMP00000166071, OTTHUMP00000166072, OTTHUMP00000174476, OTTHUMP00000174477, OTTHUMP00000222080, Oncogen ERBB, Oncogene AXL, Oncogene MET, Oncogene SRC, PDGF Receptor alpha, PDGF alpha chain, PDGF-R-alpha, PDGFR 2, PDGFRA, PDGFRA/BCR fusion, PGFRA_HUMAN, PIG61, PPP1R47, PPP1R48, PTK 3, PTK 3A protein tyrosine kinase 3A, PTK3A, Platelet derived growth factor receptor, Platelet derived growth factor receptor 2, Platelet derived growth factor receptor alpha, Platelet derived growth factor receptor alpha polypeptide, Protein phosphatase 1 regulatory subunit 48, Protein phosphatase 1, regulatory subunit 47, Protein-tyrosine kinase 3A, Protein-tyrosine kinase RTK-6, Protein-tyrosine kinase receptor flk-1, Proto oncogene tyrosine protein kinase MER, Proto oncogene tyrosine protein kinase MER precursor, Proto-oncogene c-ErbB-1, Proto-oncogene c-Mer, Proto-oncogene c-Met, Proto-oncogene c-Src, Proto-oncogene tyrosine-protein kinase Src, Protooncogene SRC, Protooncogene SRC Rous sarcoma, RCCP2, RHEPDGFRA, RP38, RSE, RTK 6, Rearranged in hypereosinophilia platelet derived growth factor receptor alpha fusion protein, Receptor type tyrosine protein kinase FLT3, Receptor tyrosine kinase MerTK, Receptor tyrosine kinase NEP, Receptor tyrosine-protein kinase ErbB-1, Rek, SA7, SF receptor, SKY, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, STK kinase, STK-1, STK12, STK15, STK5, STK6, STK6_HUMAN, STK7, Scatter factor receptor, Serine/theronine kinase 12, Serine/threonine kinase 15, Serine/threonine kinase 6, Serine/threonine-protein kinase 12, Serine/threonine-protein kinase 15, Serine/threonine-protein kinase 6, Serine/threonine-protein kinase aurora-A, Serine/threonine-protein kinase aurora-B, Species antigen 7, Stem cell tyrosine kinase 1, TCRZ, TFG/ALK, TRK E, TYRO3 protein tyrosine kinase, TYRO3_HUMAN, Tif, Tyro7, Tyrosine kinase DDR, Tyrosine kinase growth factor receptor, Tyrosine kinase pp60c src, Tyrosine kinase receptor E, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase CAK, Tyrosine-protein kinase DTK, Tyrosine-protein kinase Mer, Tyrosine-protein kinase Met, Tyrosine-protein kinase RSE, Tyrosine-protein kinase SKY, Tyrosine-protein kinase TIF, Tyrosine-protein kinase byk, Tyrosine-protein kinase receptor FLT3, Tyrosine-protein kinase receptor TYRO3, Tyrosine-protein kinase receptor UFO, UFO_HUMAN, Urogastrone, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), VEGFR, VEGFR-2, VGFR2_HUMAN, Vascular endothelial growth factor receptor 2, Wa5, anaplastic lymphoma kinase (Ki-1), anaplastic lymphoma receptor tyrosine kinase, c mer proto oncogene tyrosine kinase, c met, c-mer, erb-b2 receptor tyrosine kinase 1, hARK1, mENA, mutant anaplastic lymphoma kinase, nmf12, p60-Src, p60c-src, pp60c-src, protein tyrosine kinase 3, soluble VEGFR2, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2