|2-氯-6-甲基-N'-(4-甲基-3-(喹啉-3-基乙炔基)苯甲酰基)苯甲酰肼|CsnPharm

CAS No.: 1388803-90-4

Synonyms: K0706;SCO-088;SUN K706

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400-920-2911

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描述BCR-ABL1 plays a key role in the pathogenesis of chronic myeloid leukemia (CML), and it has been investigated as a druggable target of tyrosine kinase inhibitors (TKIs) over two decades^[1].Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively. K0706 was designed as a BCR-ABL1 TKI to provide an option for patients experiencing resistance or intolerance to the first-line TKIs imatinib, nilotinib, dasatinib, and bosutinib^[2].Potent inhibition of BCR-ABL1 tyrosine autophosphorylation by K0706 as well as inhibition of BCR-ABL1L248R, BCR-ABL1Y253H and BCR-ABL1E255V at high concentrations of inhibitor. BCR-ABL1T315I was not inhibited to a level reaching the IC50 at any of the tested concentrations of K0706^[3].
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