Chemical Structure : Relcobatinib
CAS No.:
2767305-95-1
Relcobatinib
(ELVN-001, ELVN001)
Catalog No.: PC-26352Not For Human Use, Lab Use Only.
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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377.41
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Formula
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C18H12D6FN5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Cyclopropanecarboxamide, N-[2-[4,6-di(methoxy-d3)-5-pyrimidinyl]-1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl]-2-fluoro-, (1S,2S)-
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References
1. Stefan D Gross, et al. Blood (2022) 140 (Supplement 1): 3095–3096.
2. Patent WO2022076975 A1.
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