{{cart_num}}
My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > SpebrutinibCAS：1202757-89-8
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to brown Solid
Qty：
Size：
| CAS | 1202757-89-8 |
| Name | Spebrutinib |
| Molecular Formula | C22H22FN5O3 |
| Molecular Weight | 423.44 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to brown Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25976876 |
| SMILES | COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1 |
| Target Point | Btk |
| Passage | Protein Tyrosine Kinase/RTK;Angiogenesis |
| Background | Spebrutinib is a highly selective Btk inhibitor. |
| Biological Activity | Spebrutinib 是共价，高选择性和口服活性的 Btk 抑制剂，IC50 为0.5 nM。[1] |
| In Vitro | 大量分析显示，Ramos细胞中Spebrutinib剂量反应的Btk占有率EC50(EC50 = 6 nM)与Spebrutinib对Btk激酶抑制的细胞EC50直接相关(EC50 = 8 nM)。此外，Spebrutinib抑制Ramos细胞中90％Btk活性的浓度为35 nM，而90％Btk占据所需的Spebrutinib浓度为39 nM [1]。 |
| Cell Experiment | 将细胞在无血清RPMI培养基中孵育1-1.5小时。将分离的人B细胞与Spebrutinib一起孵育，终浓度为0.001，0.01，0.1和1μM。将Ramos细胞与0.1nM-3μMSpebrutinib一起温育。然后将细胞在化合物存在下于37℃温育1小时。孵育后，将细胞离心并重悬于100μL无血清RPMI中，并加入5μg/mLα-人IgM刺激BCR。将样品离心，在磷酸盐缓冲盐水(PBS)中洗涤，并在100μL细胞提取缓冲液加1:10(v/v)PhosSTOP磷酸酶抑制剂和1:10(v/v)完全蛋白酶抑制剂中裂解[1]。 |
| Data Literature Source | [1]. Evans EK，et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
Spebrutinib是高选择性的 Btk 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Sorry, there is no more information.
Sorry, there is no more information.
Manual Download
