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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > BafetinibCAS：859212-16-1
Molecular Formula：C30H31F3N8O
Molecular Weight：576.62
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥99%
Appearance：Light yellow to yellow Solid
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| CAS | 859212-16-1 |
| Name | Bafetinib |
| Molecular Formula | C30H31F3N8O |
| Molecular Weight | 576.62 |
| Solubility | Soluble in DMSO |
| Purity | ≥99% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00008999 |
| SMILES | O=C(C1=CC=C(C(C(F)(F)F)=C1)CN2C[C@@H](N(C)C)CC2)NC3=CC=C(C)C(NC4=NC=CC(C5=CN=CN=C5)=N4)=C3 |
| Target Point | Bcr-Abl |
| Passage | Protein Tyrosine Kinase/RTK |
| Background | Bafetinib is a Lyn/Bcr-Abl tyrosine kinase inhibitor. |
| Biological Activity | Bafetinib (INNO-406, NS-187) 是一种有效的，选择性的，双重Bcr-Abl/Lyn双重抑制剂，无细胞试验中IC50为5.8 nM/19 nM，对T315I突变型的磷酸化没有抑制作用，对PDGFR和c-Kit的作用效果较弱。[1-3] |
| IC50 | Abl:5.8nM(Cell-free assay);Lyn: 19nM(Cell-free assay)[1] |
| In Vitro | Bafetinib抑制Abl和Lyn，IC50分别为5.8 nM和19 nM。此外，Bafetinib抑制WT Bcr-Abl自磷酸化，也抑制其下游激酶活性，作用于K562和293T 细胞时，IC50分别为11 nM 和 22 nM。在体外，Bafetinib 抑制Bcr-Abl阳性细胞系生长，包括K562，KU812，和BaF3/wt 细胞，而对Bcr-Abl-阴性U937 细胞系增殖没有作用效果。而且，Bafetinib作用于 Bcr-Abl点突变细胞系，如 BaF3/E255K细胞，具有抗增殖效果，这种作用具有剂量依赖性。[1] Bafetinib作用于Bcr-Abl+白血病细胞系，通过抑制Bcr-Abl磷酸化，诱导caspase调节的和caspase非依赖的细胞死亡。[2] |
| In Vivo | Bafetinib每天按 0.2 mg/kg剂量作用于Bcr-Abl阳性KU812小鼠模型，显著抑制肿瘤生长，按 20 mg/kg剂量处理，完全抑制肿瘤生长，且没有副作用。Bafetinib 按30 mg/kg剂量作用于Balb/c小鼠，所具有的药物动力学参数如下: Tmax，2小时;最大浓度值，661 ng/mL; T1/2，1小时; 最大耐药剂量，200 mg/kg/d；生物药效率(BA)，32%。[1] |
| Cell Experiment | Animal Models: 通过皮下注射KU812细胞到Balb/c-nu/nu 雌鼠的右侧而建立KU812移植瘤; Dosages: ≤20 mg/kg/day; Administration: 口服处理[1] |
| Animal Experiment | K562，BaF3/wt，BaF3/E255K，和BaF3/T315I 细胞按每孔1×103个细胞一式三份接种在96孔板上，而 KU812和U937 细胞按每孔5×103个细胞一式三份接种在96孔板上。细胞与梯度稀释的Bafetinib 温育3天。通过MTT检测实验测定细胞增殖，拟合对数曲线数据，计算IC50值。[1] |
| Data Literature Source | [1] Kimura S，et al. Blood. 2005，106(12)，3948-3954. [2] Kamitsuji Y，et al. Cell Death Differ. 2008，15(11)，1712-2172. [3] Yokota A，et al. Blood. 2007，109(1)，306-314. |
| Unit | Bottle |
| Specification | 5mg 25mg 50mg |
Bafetinib是Lyn/Bcr-Abl 酪氨酸激酶抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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