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Bafetinib

Cat. No. M1991
Bafetinib Structure
Synonym:

INNO-406, NS-187

Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 120  USD120 In stock
50mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM and 19 nM, respectively. 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 (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day in Bcr-Abl-positive KU812 mouse model. Bafetinib (NS-187) inhibited both Tyr393-phosphorylated and Tyr393-unphosphorylated Abl, resulting in significant in vitro growth inhibition of cells expressing six of seven mutated Bcr-Abl kinases, though not T315I. Furthermore, Bafetinib (INNO-406) prolonged the survival of mice injected with leukemic cells expressing all mutated Bcr-Abl tested except T315I, and its efficacy correlated well with its in vitro effects. INNO-406 (formerly NS-187) is 25 to 55 times more potent than imatinib mesylate in vitro and at least 10 times more potent in vivo. Bafetinib is currently in Phase II clinical trials in patients with hormone refractory prostate cancer.

Chemical Information
Molecular Weight 576.62
Formula C30H31F3N8O
CAS Number 859212-16-1
Solubility (25°C) DMSO 110 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Santos FP, et al. Curr Opin Investig Drugs. Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia.

[2] Yokota A, et al. Blood. 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.

[3] Naito H, et al. Leuk Res. In vivo antiproliferative effect of NS-187, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor, on leukemic cells harbouring Abl kinase domain mutations.

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Keywords: Bafetinib, INNO-406, NS-187 supplier, Src-bcr-Abl, inhibitors, activators


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