2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor c-Met/HGFR
  4. Glesatinib

Glesatinib  (Synonyms: MGCD265)

目录号: HY-19642
产品使用指南

摩尔计算器

Glesatinib (MGCD265) 是一种具有口服活性的，有效的 MET/SMO 双抑制剂。 Glesatinib 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)。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Glesatinib hydrochloride 通常具有更好的水溶性和稳定性。

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Glesatinib Chemical Structure

Glesatinib Chemical Structure

CAS No. : 936694-12-1

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Glesatinib 的其他形式现货产品:

Customer Review

Other Forms of Glesatinib:

Glesatinib 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC)[1][2].

体外研究
(In Vitro)

Glesatinib (MGCD265; 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[1].
Glesatinib (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells[1].
Glesatinib 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[1].
Glesatinib (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp[2].
Glesatinib (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner[2].

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

Glesatinib 相关抗体:

Cell Proliferation Assay[1]

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 (MGCD265; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].

MCE 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[1]
Dosage: 15 mg/kg
Administration: Orally; daily; 40 weeks
Result: Caused a significant decrease in tumor size.
Clinical Trial
分子量

619.70

Formula

C31H27F2N5O3S2
CAS 号
中文名称

葛雷沙替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Glesatinib 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Glesatinib936694-12-1MGCD265葛雷沙替尼MGCD 265MGCD-265TAM Receptorc-Met/HGFRTyro3AxlMerorallyMETSMOtyrosinekinaseP-glycoproteinP-gpmultidrugresistanceMDRnon-smallcelllungcancerNSCLCInhibitorinhibitorinhibit

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