Vodobatinib (K0706) 是一种有效的第三代，且具有口服活性的 Bcr-Abl1 酪氨酸激酶抑制剂，IC50 为 7 nM。Vodobatinib 对大多数 BCR-ABL1 点突变体具有活性，对 BCR-ABL1T315I 无活性。 Vodobatinib 可用于慢性粒细胞白血病 (CML) 研究。
货号:ajcx33058
CAS:1388803-90-4
分子式:C27H20ClN3O2
分子量：453.92
溶解度:DMSO : 125 mg/mL (275.38 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research[1][2].

In Ba/F3 cells expressing BCR-ABL1, BCR-ABL1L248V, BCR-ABL1Y253H, or BCR-ABL1E255V, Vodobatinib (K0706; 0-2000 nM) treatment shows potent inhibition of BCR-ABL1 tyrosine autophosphorylation[1].

[1]. Orlando Antelope, et al. BCR-ABL1 tyrosine kinase inhibitor K0706 exhibits preclinical activity in Philadelphia chromosome-positive leukemia. Exp Hematol. 2019 Sep;77:36-40.e2.
[2]. Phase 1 Trial of Vodobatinib, a Novel Oral BCR-ABL1 Tyrosine Kinase Inhibitor (TKI): Activity in CML Chronic Phase Patients Failing TKI Therapies Including Ponatinib. Session: 632: Chronic Myeloid Leukemia: Therapy: CML: New and Beyond.