1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. Bcr-Abl
    Autophagy

Bafetinib (Synonyms: INNO-406; NS-187)

Cat. No.: HY-50868 Purity: 99.27%
Data Sheet SDS Handling Instructions

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays.

For research use only. We do not sell to patients.
Bafetinib Chemical Structure

Bafetinib Chemical Structure

CAS No. : 859212-16-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $95 In-stock
5 mg $75 In-stock
10 mg $130 In-stock
50 mg $390 In-stock
100 mg $480 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays. IC50 value: 5.8 nM/19 nM [2] Target: Bcr-Abl/Lyn in vitro: Bafetinib (1-10 μM) concentration dependently inhibits PAR2-TRPV4 coupling. In TRPV4 HEKs, 10 μM Bafetinib significantly inhibits the coupling response to SLIGRL and trypsin compared with vehicle control. Bafetinib inhibits the signalling pathway leading to TRPV4 channel opening, downstream of PAR2 activation, most likely by blocking the activation of a tyrosine kinase. [1] 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. [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%.[2]

Clinical Trial
View MoreCollapse
References
Molecular Weight

576.62

Formula

C₃₀H₃₁F₃N₈O

CAS No.

859212-16-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 42 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Bafetinib
Cat. No.:
HY-50868
Quantity: