For research use only. Not for therapeutic Use.
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]. Vodobatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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].
| Catalog Number | I038095 |
| CAS Number | 1388803-90-4 |
| Synonyms | 2-chloro-6-methyl-N’-[4-methyl-3-(2-quinolin-3-ylethynyl)benzoyl]benzohydrazide |
| Molecular Formula | C27H20ClN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H20ClN3O2/c1-17-10-12-22(26(32)30-31-27(33)25-18(2)6-5-8-23(25)28)15-20(17)13-11-19-14-21-7-3-4-9-24(21)29-16-19/h3-10,12,14-16H,1-2H3,(H,30,32)(H,31,33) |
| InChIKey | ZQOBVMHBVWNVBG-UHFFFAOYSA-N |
| SMILES | CC1=C(C(=CC=C1)Cl)C(=O)NNC(=O)C2=CC(=C(C=C2)C)C#CC3=CC4=CC=CC=C4N=C3 |
| Reference | [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. |
