- Bafetinib
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2026-06-03
- CAS:859212-16-1
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 20tons
- Bafetinib
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- $31.00
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2026-05-11
- CAS:859212-16-1
- Purity: 98.02%
- Supply Ability: 10g
- Bafetinib USP/EP/BP
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- $1.10
-
2025-11-18
- CAS:859212-16-1
- Min. Order: 1g
- Purity: 99.9%
- Supply Ability: 100 Tons Min
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| | 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;Unii-nvw4Z03I9b;Bafetinib (INNO-406);N-[3-([4,5'-BipyriMidin]-2-ylaMino)-4-Methylphenyl]-4-[[(3S)-3-(diMethylaMino)-1-pyrrolidinyl]Methyl]-3-(trifluoroMethyl)benzaMide | | CAS: | 859212-16-1 | | MF: | C30H31F3N8O | | MW: | 576.62 | | EINECS: | | | 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 |
| | Bafetinib Preparation Products And Raw materials |
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