Glesatinib hydrochloride|1123838-51-6|(MGCD265 hydrochloride)-陌孚医药/Medlife

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Glesatinib hydrochloride (Synonyms: MGCD265 hydrochloride)

目录号: PL04914 纯度: ≥98%

CAS No. :1123838-51-6

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中文名称	Glesatinib hydrochloride
中文别名	葛雷沙替尼盐酸盐
英文名称	Glesatinib hydrochloride
英文别名	Glesatinib (hydrochloride);MGCD265 hydrochloride;MGCD-265 hydrochloride;Glesatinib hydrochloride;Glesatinib HCl;N-[[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-(4-fluorophenyl)acetamide;hydrochloride;Glesatinib hydrochloride; MGCD265 hydrochloride;N-((3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-(4-fluorophenyl)acetamide hydrochloride
Cas No.	1123838-51-6
分子式	C₃₁H₂₈ClF₂N₅O₃S₂
分子量	656.17
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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).

性状

Solid

体外研究(In Vitro)

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 [H]-Paclitaxel accumulation and inhibits [H]-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.

体内研究(In Vivo)

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Morgillo F, et al. Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-7458.
[2]. Cui Q, et al. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated MultidrugResistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313.

溶解度数据	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

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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