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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > BMS-935177CAS：1231889-53-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 1231889-53-4 |
| Name | BMS-935177 |
| Molecular Formula | C31H26N4O3 |
| Molecular Weight | 502.56 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | O=C(C1=CC=C(C2=CC=CC(N3C=NC4=C(C=CC=C4)C3=O)=C2C)C5=C1NC6=C5C=CC(C(C)(O)C)=C6)N |
| Target Point | Btk |
| Passage | Protein Tyrosine Kinase/RTK;Angiogenesis |
| Background | BMS-935177 is a potent and reversible BTK inhibitor. |
| Biological Activity | BMS-935177是一种有效的、可逆的BTK抑制剂，IC50为2.8 nM，具有良好的激酶选择性。它对BTK比对其他激酶如TEC, BMX, ITK, and TXK更有效力，选择性是其5-67倍。[1] |
| IC50 | BTK(Cell-free assay):2.8nM;BLK(Cell-free assay):20nM;BMX(Cell-free assay):24nM[1] |
| In Vitro | BMS-935177对BTK的选择性比对SRC激酶家族成员高50倍以上。在Ramos B细胞中，BMS-935177抑制钙流动；在受到anti-IgM和anti-IgG刺激的外周血b淋巴细胞中，BMS-935177抑制CD69的细胞表面表达。但在受到CD40受体和配体刺激的B细胞中，BMS-935177对CD69的表达无影响。在PBMCs中，BMS-935177可有效地抑制TNF-α的生成，IC50为14 nM[1]。 |
| In Vivo | 在多种检测物种中，BMS-935177的血浆蛋白结合率高，在人体中，游离药物比率小于1%。在临床前检测中，无论是悬浮物还是溶液形式给药，BMS-935177具有良好的口服活性，尽管其水溶性差。以溶液形式给药，BMS-935177在大鼠、小鼠、狗、和食蟹猴中的口服生物利用度为84%-100%，而在单次静脉注射给药实验中，具有较低的体内清除率。在小鼠和大鼠中静脉注射2 mg/kg的剂量，BMS-935177的T1/2分别为4 h和5.1 h[1]。 |
| Data Literature Source | [1] De Lucca GV，et al. J Med Chem. 2016，59(17):7915-35. |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
BMS-935177是一种有效的、可逆的BTK抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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