CHMFL-BMX-078 CHMFL-BMX 078|cas:1808288-51-8|西域试剂

CHMFL-BMX-078 CHMFL-BMX 078,98.0%

产品编号：Bellancom-101267| CAS NO：1808288-51-8| 分子式：C₃₃H₃₅N₇O₆| 分子量：625.67

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101267	￥2400.00	杭州北京（现货）
Bellancom-101267	￥3800.00	杭州北京（现货）
Bellancom-101267	￥12000.00	杭州北京（现货）
Bellancom-101267	￥18000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

CHMFL-BMX-078 CHMFL-BMX 078

产品介绍

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。

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.

体外研究

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 K_d of 81 nM, while for the active state of BMX kinase, it exhibits a binding K_d 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

CHMFL-BMX-078 exhibits a short half-life (T_1/2=0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable C_max (13565.23 ng/mL) and AUC_0-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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (47.95 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5983 mL	7.9914 mL	15.9829 mL
5 mM	0.3197 mL	1.5983 mL	3.1966 mL
10 mM	0.1598 mL	0.7991 mL	1.5983 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。