上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
CHMFL-BMX-078 (Synonyms: CHMFL-BMX 078) 纯度: ≥98.0%
CHMFL-BMX-078是高效的,选择性的,不可逆的,类型II BMX激酶抑制剂,IC50值为11 nM。
CHMFL-BMX-078 Chemical Structure
CAS No. : 1808288-51-8
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥4818 | In-stock | |
1 mg | ¥1200 | In-stock | |
5 mg | ¥3500 | In-stock | |
10 mg | ¥5500 | In-stock | |
50 mg | ¥16500 | In-stock | |
100 mg | ¥22500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
CHMFL-BMX-078 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Protein Tyrosine Kinase Compound Library
- Anti-Cancer Compound Library
- Covalent Screening Library
- Targeted Diversity Library
生物活性 |
CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM. |
IC50 & Target |
IC50: 11 nM (BMX)[1] |
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体外研究 (In Vitro) |
Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC50=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding Kd of 81 nM, while for the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI50=0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC50=5.8 nM) than C496S mutant (EC50=459 nM) for the inhibition of BMX total tyrosine phosphorylation. CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
CHMFL-BMX-078 exhibits a short half-life (T1/2=0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable Cmax (13565.23 ng/mL) and AUC0-t (1386.41 ng/mL h) in iv injection. However, it is not absorbed by oral administration, indicating that this compound could be administrated through iv or ip injection when used as a research tool[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
625.67 |
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Formula |
C33H35N7O6 |
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CAS 号 |
1808288-51-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 30 mg/mL (47.95 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
The kinase reaction system contains BMX or BTK, 1 μL of serially diluted CHMFL-BMX-078, and substrate Poly peptidewith 100 μM ATP. The reaction in each tube is started immediately by adding ATP and kept going for an hour under 37 °C. After the tube cooled for 5 min at room temperature, 5 μL solvent reactions are carried out in a 384-well plate. Then 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ATP within 40 min. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 30 min to produce a luminescence signal. Luminescence signal is measured with an automated plate reader[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Rats: Six 8-week-old male Sprague−Dawley rats are fasted overnight before starting drug treatment via intravenous and oral administration. Animal blood collection time points are as follows. For groups 1, 3, and 5 (intravenous): 1 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h before and after administration is selected. For group 2, 4, and 6 (oral): 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h before and after dosing. The plasma is collected for analysis[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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