Glesatinib hydrochloride MGCD265 hydrochloride|cas:1123838-51-6|西域试剂

Glesatinib hydrochloride MGCD265 hydrochloride,98.0%

产品编号：Bellancom-19642A| CAS NO：1123838-51-6| 分子式：C₃₁H₂₈ClF₂N₅O₃S₂| 分子量：656.17

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货号	价格	库存与货期
Bellancom-19642A	￥3200.00	杭州北京（现货）
Bellancom-19642A	￥4500.00	杭州北京（现货）
Bellancom-19642A	￥9000.00	杭州北京（现货）
Bellancom-19642A	￥15000.00	杭州北京（现货）
Bellancom-19642A	￥21000.00	杭州北京（现货）

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Glesatinib hydrochloride MGCD265 hydrochloride

产品介绍

Glesatinib hydrochloride (MGCD265 hydrochloride) 是一种具有口服活性的，有效的 MET/SMO 双抑制剂。 Glesatinib hydrochloride 是一种酪氨酸激酶抑制剂，可拮抗非小细胞肺癌 (NSCLC) 中 P 糖蛋白介导的多药耐药性 (MDR)。

生物活性

Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

体外研究

Glesatinib hydrochloride (MGCD265 hydrochloride; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC₅₀ value of 0.08 μM on NSCLC H1299 cells.
Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells.
Glesatinib hydrochloride has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC₅₀s fell between 5 and 10 μM.
Glesatinib hydrochloride (1, 3 μM; 120 mins) increases the intracellular [³H]-Paclitaxel accumulation and inhibits [³H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp.
Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner.

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

Cell Proliferation Assay

Cell Line:	NSCLC H1299 cells
Concentration:	0.01, 0.1, 1, 2, 5 μM
Incubation Time:	For 72 hours
Result:	Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC₅₀ value of 0.08 μM.

体内研究
(In Vivo)

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size.

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

Animal Model:	4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts
Dosage:	15 mg/kg
Administration:	Orally; daily; 40 weeks
Result:	Caused a significant decrease in tumor size.

体内研究

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size.

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

Animal Model:	4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts
Dosage:	15 mg/kg
Administration:	Orally; daily; 40 weeks
Result:	Caused a significant decrease in tumor size.

体内研究

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size.

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

Animal Model:	4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts
Dosage:	15 mg/kg
Administration:	Orally; daily; 40 weeks
Result:	Caused a significant decrease in tumor size.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (76.20 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5240 mL	7.6200 mL	15.2400 mL
5 mM	0.3048 mL	1.5240 mL	3.0480 mL
10 mM	0.1524 mL	0.7620 mL	1.5240 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 (sealed storage, away from moisture)。-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 (3.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.81 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.81 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.81 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。