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INNO 406
- Bafetinib
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C30H31F3N8O
- MW: 576.62
Description
INNO 406 (Bafetinib) is an orally bioavailable dual Bcr-Abl and Lyn kinase inhibitor with anti-CML activity. It is reported to be more than 10-fold more potent than imatinib in relevant Abl-dependent assay systems.
Bcr-Abl drives chronic myeloid leukemia, while Lyn signaling contributes to leukemic cell survival and some resistance phenotypes. INNO 406 is a useful pharmacological tool for CML kinase biology and Abl/Lyn inhibitor comparison.
Key Features
- Dual Bcr-Abl and Lyn kinase inhibitor
- Orally bioavailable kinase inhibitor scaffold
- Potent activity in CML-relevant systems
- Useful comparator to imatinib-sensitive and resistant models
Applications
- Bcr-Abl kinase assays
- Chronic myeloid leukemia research
- Lyn kinase signaling studies
- Tyrosine kinase inhibitor profiling
More Information
| Parent CAS No. | 859212-16-1 |
|---|---|
| Chemical Name | (S)-N-(3-(4,5'-bipyrimidin-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide |
| SMILES | C1N=C(NC2C(C)=CC=C(NC(=O)C3C=C(C(F)(F)F)C(CN4C[C@H](CC4)N(C)C)=CC=3)C=2)N=C(C2C=NC=NC=2)C=1 |&1:24,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C30H31F3N8O/c1-19-4-7-23(13-27(19)39-29-36-10-8-26(38-29)22-14-34-18-35-15-22)37-28(42)20-5-6-21(25(12-20)30(31,32)33)16-41-11-9-24(17-41)40(2)3/h4-8,10,12-15,18,24H,9,11,16-17H2,1-3H3,(H,37,42)(H,36,38,39)/t24-/m0/s1 |
| InChiKey | ZGBAJMQHJDFTQJ-DEOSSOPVSA-N |
| CID | 11387605 |
| Short Description | Bcr-Abl/Lyn inhibitor |
References
- A Yokota et al. INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity. Blood, 2007, 109(1), 306-314.
- H Kantarjian et al. Phase 1 study of INNO-406, a dual Abl/Lyn kinase inhibitor, in Philadelphia chromosome-positive leukemias after imatinib resistance or intolerance. Cancer, 2010, 116(11), 2665-72.
- JC Uitdehaag et al. A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets. Br. J. Pharmacol. 2012, 166, 858–876.
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