Relcobatinib | ABL1 inhibitor | Probechem Biochemicals

Chemical Structure : Relcobatinib

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Relcobatinib (ELVN-001, ELVN001)

货号: PC-26352Not For Human Use, Lab Use Only.

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生物&药学活性

Relcobatinib (ELVN-001) is a potent, selective and ATP-competitive inhibitor of ABL1 kinase, shows activity againsst clinically relevant BCR-ABL1 TKI-resistant mutants T315I as well as myristoyl pocket mutants (A334P, P465S), which are highly resistant to asciminib.
Relcobatinib (ELVN-001) is highly selective in both biochemical and cell-based assays versus the kinome in general as well as the key off-target kinases KDR, c-KIT, PDGFR and SRC.
ELVN-001 exhibited potent pharmacodynamic (phosphorylated CRKL) and anti-proliferative activity in vitro against BCR-ABL1-driven CML cell lines.
ELVN-001 reduces outgrowth of resistant clones in cell-based mutagenesis screens using Ba/F3 BCR-ABL1 cells.
ELVN-001 demonstrated efficacy in vivo tumor xenograft models, including a model of T315I CML.

物理化学性质&存储条件

分子量	377.41
分子式	C18H12D6FN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Cyclopropanecarboxamide, N-[2-[4,6-di(methoxy-d3)-5-pyrimidinyl]-1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl]-2-fluoro-, (1S,2S)-

参考文献

1. Stefan D Gross, et al. Blood (2022) 140 (Supplement 1): 3095–3096.

2. Patent WO2022076975 A1.

Relcobatinib (ELVN-001, ELVN001)

生物&药学活性

物理化学性质&存储条件

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Relcobatinib (ELVN-001, ELVN001)

生物&药学活性

物理化学性质&存储条件

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