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Bafetinib

巴非替尼,NS-187,NS 187,NS187,INNO 406,INNO-406,INNO406

Bafetinib (INNO-406)是一种有效的，选择性的，Bcr-Abl/Lyn双重抑制剂，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的作用效果稍弱。

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生物活性

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, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.
体外研究
体内研究
激酶实验
细胞实验

0- 10 μM
动物实验

≤20 mg/kg/day口服处理
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Kimura S, et al. Blood. 2005, 106(12), 3948-3954.

分子式 C30H31F3N8O	分子量 576.62	CAS号 859212-16-1	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO 100 mg/mL	Water <1 mg/mL	Ethanol <1 mg/mL

体内溶解度

NCT Number	Conditions	Interventions	Sponsor/Collaborators	Phases	Start Date	Last Updated
NCT01215799	Hormone Refractory Prostate Cancer	Drug: Bafetinib	CytRx	Phase 2	2010-08-01	2011-12-14
NCT01144260	B-Cell Chronic Lymphocytic Leukemia	Drug: bafetinib	CytRx	Phase 2	2010-06-01	2013-05-14
NCT01234740	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	Drug: bafetinib\|Procedure: microdialysis\|Other: pharmacological study\|Other: liquid chromatography\|Other: mass spectrometry\|Other: laboratory biomarker analysis\|Genetic: protein expression analysis\|Genetic: western blotting\|Other: immunohistochemistry staining method\|Procedure: therapeutic conventional surgery	City of Hope Medical Center\|National Cancer Institute (NCI)		2010-12-01	2013-03-18
NCT00352677	Chronic Myeloid Leukemia\|Acute Lymphocytic Leukemia	Drug: INNO-406	CytRx	Phase 1	2006-07-01	2009-05-29
NCT00469534	High Grade Glioma	Procedure: IMRT	Alberta Health Services\|AHS Cancer Control Alberta			2011-09-21
NCT00330109	Glioma	Procedure: MRS Imaging\|Procedure: PET Scanning\|Procedure: Diffusion Tensor Imaging	AHS Cancer Control Alberta		2006-06-01	2017-01-13

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。