• We specialize in small molecule inhibitors, agonists, antagonists and screening libraries!
Search Site
Home >> Signaling Pathways >> TGF-β / Smad Signaling >> Bcr-Abl >> Bafetinib (INNO-406)
Related Products
Bafetinib (INNO-406)Bcr-Abl/Lyn tyrosine kinase inhibitor

Bafetinib (INNO-406)

Catalog No. B1011
Size Price Stock Qty
10mM (in 1mL DMSO) $130.00 In stock
5mg $75.00 In stock
10mg $139.00 In stock
25mg $243.00 In stock
100mg $488.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Sterne, Gabriella R., Jung Hwan Kim, and Bing Ye. "Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors." eLife 4 (2015): e05196. PMID:25988807

Quality Control

Chemical structure

Bafetinib

Related Biological Data

Bafetinib

Biological Activity

Description Bafetinib (INNO-406) is an orally bioavailable, dual inhibitor of Bcr-Abl and Lyn-kinase with IC50 value of 5.8 nM/19 nM, respectively.
Targets Abl Lyn        
IC50 5.8 nM 19 nM        

Protocol

Kinase experiment [1]:

Kinase assays

Bcr-Abl kinase assays were 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 was used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn were carried out with an enzyme-linked immunosorbent assay (ELISA) kit from Carna Biosciences.

Cell experiment [1]:

Cell lines

K562, BaF3/wt and KU812 cell lines

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-10 μM for 3 days

Applications

Bafetinib could suppress the growth of the Bcr-Abl–positive cell lines K562, KU812, and BaF3/wt.

Animal experiment [1]:

Animal models

Bcr-Abl–positive KU812 mouse model

Dosage form

0.2 mg/kg/d and 20 mg/kg/d orally twice a day for 26 consecutive days

Application

Bafetinib suppressed the growth of Bcr-Abl–bearing tumors (KU812) and markedly extends the survival of mice bearing such tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.

Bafetinib (INNO-406) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Bafetinib (INNO-406) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 887650-05-7 SDF Download SDF
Chemical Name 4-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(5-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide
Canonical SMILES CC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CCC(C3)N(C)C)C(F)(F)F)NC4=NC=C(C=N4)C5=CN=CN=C5
Formula C30H31F3N8O M.Wt 576.62
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Bafetinib is a potent and selective dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC50 values of 5.8nM and 19nM, respectively [1].

Bafetinib is a specific dual Abl-Lyn inhibitor. For 79 other tyrosine kinases, 0.1μM bafetinib can inhibit 4 of these enzymes including Abl, Abl-related gene, Fyn and Lyn. Bafetinib can block the autophosphorylation of Bcr-Abl. In K562 and 293T cells transfected with wt Bcr-Abl, bafetinib shows inhibition with IC50 values of 11nM and 22nM, respectively. In the in vitro kinase assays, bafetinib shows inhibition of a variety of Abl kinase mutants such as M244V, G250E, Y253F and F317L. It has no effect on T315I in vitro. Bafetinib also suppresses the growth of Bcr-Abl–positive leukemic cell lines including K562, KU812 and BaF3/wt. The BaF3/E255K cells are also sensitive towards bafetinib. Moreover, bafetinib is highly potent to inhibit tumor growth in murine tumor models [1].

References:
[1] Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.