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.

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Bafetinib Chemical Structure

Bafetinib Chemical Structure

CAS No. : 859212-16-1

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10 mM * 1 mL in DMSO $95 In-stock
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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
NCT Number Sponsor Condition Start Date Phase
NCT01215799 CytRx Hormone Refractory Prostate Cancer August 2010 Phase 2
NCT01144260 CytRx B-Cell Chronic Lymphocytic Leukemia June 2010 Phase 2
NCT01234740 City of Hope Medical Center|National Cancer Institute (NCI) Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor|Tumors Metastatic to Brain|Adult Anaplastic Oligoastrocytoma December 2010
NCT01215799 CytRx Hormone Refractory Prostate Cancer August 2010 Phase 2
NCT01144260 CytRx B-Cell Chronic Lymphocytic Leukemia June 2010 Phase 2
NCT01234740 City of Hope Medical Center|National Cancer Institute (NCI) Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor|Tumors Metastatic to Brain|Adult Anaplastic Oligoastrocytoma December 2010
NCT00352677 CytRx Chronic Myeloid Leukemia|Acute Lymphocytic Leukemia July 2006 Phase 1
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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.

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Bafetinib
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