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Bafetinib

Catalog No. T6311   CAS 859212-16-1
Synonyms: INNO-406, mutations, NS187, Bcr-Abl, Src, INNO 406, Bafetinib, Apoptosis, inhibit, philadelphia chromosome-positive leukemias, NS 187, Inhibitor, NS-187, INNO406

Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.

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Bafetinib, CAS 859212-16-1
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.
Targets&IC50 Abl:5.8 nM, Lyn:19 nM
In vitro Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells. [1] In Bcr-Abl+ leukemia cell lines, Bafetinib induces both caspase-mediated and caspase-independent cell death by blocking the phosphorylation of Bcr-Abl. [2]
In vivo In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone. [3]
Kinase Assay Kinase assay : Bcr-Abl kinase assays are performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase is used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn are carried out with an enzyme-linked immunosorbent assay (ELISA) kit. The inhibitory effects of NS-187 against 79 tyrosine kinases are tested with KinaseProfiler.
Cell Research K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1 × 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5 × 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve. (Only for Reference)
Synonyms INNO-406, mutations, NS187, Bcr-Abl, Src, INNO 406, Bafetinib, Apoptosis, inhibit, philadelphia chromosome-positive leukemias, NS 187, Inhibitor, NS-187, INNO406
Molecular Weight 576.62
Formula C30H31F3N8O
CAS No. 859212-16-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 93 mg/mL (161.3 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Kimura S, et al. Blood. 2005, 106(12), 3948-3954. 1. Jing Y, Dai X, Yang L, et al. STING couples with PI3K to regulate actin reorganization during BCR activation. Science Advances. 2020, 6(17): eaax9455. 2. Wu J, Nie Y, Wang J, et al. Fcγ receptor‐mediated phagocytosis pathway was involved in phagocytosis of mIgM+ B lymphocytes from largemouth bass (Micropterus salmoides). Journal of Fish Biology. 2022 2. Kamitsuji Y, et al. Cell Death Differ. 2008, 15(11), 1712-2172. 3. Yokota A, et al. Blood. 2007, 109(1), 306-314. 4. Jing Y, Dai X, Yang L, et al. STING couples with PI3K to regulate actin reorganization during BCR activation[J]. Science Advances. 2020, 6(17): eaax9455.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Autophagy Compound Library HIF-1 Signaling Pathway Compound Library TGF-beta/Smad Compound Library Hematonosis Compound Library Inhibitor Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library

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