Embibatinib (TERN-701) | BCR-ABL1 inhibitor

Chemical Structure : Embibatinib

Embibatinib (TERN-701, TERN701, HS-10382, HS10382)

Catalog No.: PC-26324Not For Human Use, Lab Use Only.

Embibatinib (TERN-701) is a potent, selective and allosteric and oral inhibitor of BCR-ABL1 tyrosine kinase inhibitor.

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Biological Activity

Embibatinib (TERN-701) is a potent, selective and allosteric and oral inhibitor of BCR-ABL1 tyrosine kinase inhibitor.

TERN-701 inhibits cell proliferation in various clinically relevant mutant CML cell lines (including T315I) with IC 50s ranging from 5 to 26 nM and 70 to 1200 nM against active site and myristoyl site mutations, respectively.

TERN-701 is highly selective for BCR::ABL1, with no appreciable activity (>50%) against >450 purified kinase targets.

TERN-701 is more selective than the comparator allosteric BCR::ABL1 inhibitor asciminib while maintaining similar potency.

TERN-701 works synergistically with multiple TKIs in the non-mutant K562 cell line.

Physicochemical Properties

M.Wt	523.87
Formula	C23H18ClF4N5O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1H-Benzimidazole-5-carboxamide, N-[4-(chlorodifluoromethoxy)phenyl]-2-(difluoromethyl)-1-[(1R)-2-hydroxy-1-methylethyl]-7-(5-pyrimidinyl)-

References

1. Patent US20200087283 A1.

Embibatinib (TERN-701, TERN701, HS-10382, HS10382)

Biological Activity

Physicochemical Properties

References

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