Bafetinib
Bafetinib Basic information
- Product Name:
- Bafetinib
- Synonyms:
-
- Benzamide, N-(3-((4,5'-bipyrimidin)-2-ylamino)-4-methylphenyl)-4-(((3S)-3-(dimethylamino)-1-pyrrolidinyl)methyl)-3-(trifluoromethyl)-
- Inno 406
- Inno-406
- 4-[[(3S)-3-Dimethylaminopyrrolidin-1-yl]methyl]-N-[4-methyl-3-[(4-pyrimidin-5-ylpyrimidin-2-yl)amino]phenyl]-3-(trifluoromethyl)benzamide
- NS-187; BAFETINIB; INNO406
- CS-239
- INNO 406 - Bafetinib
- Ns 187
- CAS:
- 859212-16-1
- MF:
- C30H31F3N8O
- MW:
- 576.62
- Product Categories:
-
- Aromatics
- Chiral Reagents
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 859212-16-1.mol
Bafetinib Chemical Properties
- Melting point:
- 166-168°C
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Refrigerator
- solubility
- DMSO:42.0(Max Conc. mg/mL);72.84(Max Conc. mM)
- form
- A crystalline solid
- pka
- 12.72±0.70(Predicted)
- color
- Light yellow to yellow
Bafetinib Usage And Synthesis
Description
Bcr-Abl, a fusion protein with deregulated tyrosine kinase activity, is highly expressed in chronic myelogenous leukemia (CML). Bafetinib is a rationally developed tyrosine kinase inhibitor based on the chemical structure of imatinib , with modifications added to improve binding and potency against Bcr-Abl kinase (IC50 = 5.8 nM). It is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo. Bafetinib inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation and also targets the Src family kinase Lyn (IC50 = 19 nM), which has been associated with resistance to imatinib in CML.
Chemical Properties
Pale Yellow Solid
Uses
A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Abl kinase inhibitor.
in vivo
Bafetinib (30 mg/kg/day, orally, for 10 consecutive days) inhibits the expression of PD-L1 in mouse lung cancer[1].
Bafetinib (10 mg/kg, gavage, single dose) alleviates pain in mice by inhibiting PAR2-induced TRPV4 channel activation[2].
| Animal Model: | Murine inflammatory pain model[2] |
| Dosage: | 10 mg/kg |
| Administration: | i.g. |
| Result: | Inhibited PAR2-induced mechanical hyperalgesia. |
References
[1] SHINYA KIMURA. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia.[J]. Blood, 2005, 106 12: 3948-3954. DOI: 10.1182/blood-2005-06-2209
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