1. Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor
  3. Sitravatinib malate

Sitravatinib malate  (Synonyms: MGCD516 malate; MG-516 malate)

目录号: HY-16961A
产品使用指南

Sitravatinib malate (MGCD516 malate) 是一种有口服活性的受体酪氨酸激酶 (RTK) 抑制剂。抑制 Axl,MER,VEGFR3,VEGFR2,VEGFR1,KIT,FLT3,DDR2,DDR1,TRKA,和 TRKBIC50 分别为 1.5 nM,2 nM,2 nM,5 nM,6 nM,6 nM,8 nM,0.5 nM,29 nM,5 nM,和 9 nM。Sitravatinib malate 单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。

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Sitravatinib malate Chemical Structure

Sitravatinib malate Chemical Structure

CAS No. : 2244864-88-6

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Sitravatinib malate 的其他形式现货产品:

Customer Review

Other Forms of Sitravatinib malate:

MCE 顾客使用本产品发表的 2 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively[1]. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].

IC50 & Target[1]

VEGFR1

6 nM (IC50)

VEGFR2

5 nM (IC50)

VEGFR3

2 nM (IC50)

TrkA

5 nM (IC50)

TrkB

9 nM (IC50)

DDR1

29 nM (IC50)

DDR2

0.5 nM (IC50)

Axl

1.5 nM (IC50)

MER

2 nM (IC50)

KIT

6 nM (IC50)

FLT3

8 nM (IC50)

体外研究
(In Vitro)

Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines[2].
Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines[2].

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

Cell Viability Assay[2]

Cell Line: KLN205, E0771, CT1B-A5 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.
体内研究
(In Vivo)

Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model[2].

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

Animal Model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells)[2]
Dosage: 20 mg/kg
Administration: Oral administration; once per day for 6 days
Result: Significantly inhibited tumor progression and induced tumor regression.
Clinical Trial
分子量

763.76

Formula

C37H35F2N5O9S

CAS 号
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
  • 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 *
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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.

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产品名称:
Sitravatinib malate
目录号:
HY-16961A
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