2. Protein Tyrosine Kinase/RTK
  3. VEGFR PDGFR c-Kit
  4. Telatinib mesylate

Telatinib mesylate  (Synonyms: Bay 57-9352 mesylate)

目录号: HY-10527C 纯度: 99.74%
COA 产品使用指南

摩尔计算器

Telatinib mesylate (Bay 57-9352 mesylate) 是一种有效的的口服活性的 VEGFR2，VEGFR3，PDGFα 和 c-Kit 抑制剂，IC50 分别为 6 nM，4 nM，15 nM 和 1 nM。

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Telatinib mesylate Chemical Structure

Telatinib mesylate Chemical Structure

CAS No. : 332013-26-0

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Customer Review

Other Forms of Telatinib mesylate:

Telatinib mesylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].

IC50 & Target[1]

VEGFR2

6 nM (IC50)

VEGFR3

4 nM (IC50)

PDGFRα

15 nM (IC50)

c-Kit

1 nM (IC50)

体外研究
(In Vitro)

Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines[2].
Telatinib at 1 μM significantly reduces the rate of [3H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [3H]-E₂17βG in ABCG2 overexpressing membrane vesicles[2].

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

Telatinib mesylate 相关抗体:
体内研究
(In Vivo)

Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[2].

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

Animal Model: Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells[2]
Dosage: 15 mg/kg
Administration: Oral dministration; every 2nd and 3rd day; total 12 times
Result: With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.
Clinical Trial
分子量

505.93

Formula

C21H20ClN5O6S
CAS 号
性状

固体

颜色

White to off-white

中文名称

甲磺酸替拉替尼；甲磺酸特拉替尼
运输条件

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

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (494.14 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9766 mL 9.8828 mL 19.7656 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Telatinib mesylate 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9766 mL 9.8828 mL 19.7656 mL 49.4140 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 mL 9.8828 mL
10 mM 0.1977 mL 0.9883 mL 1.9766 mL 4.9414 mL
15 mM 0.1318 mL 0.6589 mL 1.3177 mL 3.2943 mL
20 mM 0.0988 mL 0.4941 mL 0.9883 mL 2.4707 mL
25 mM 0.0791 mL 0.3953 mL 0.7906 mL 1.9766 mL
30 mM 0.0659 mL 0.3294 mL 0.6589 mL 1.6471 mL
40 mM 0.0494 mL 0.2471 mL 0.4941 mL 1.2353 mL
50 mM 0.0395 mL 0.1977 mL 0.3953 mL 0.9883 mL
60 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
80 mM 0.0247 mL 0.1235 mL 0.2471 mL 0.6177 mL
100 mM 0.0198 mL 0.0988 mL 0.1977 mL 0.4941 mL
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:

Telatinib332013-26-0Bay 57-9352甲磺酸替拉替尼甲磺酸特拉替尼VEGFRPDGFRc-KitVascular endothelial growth factor receptorPlatelet-derived growth factor receptorSCFRCD117VEGFR2VEGFR3PDGFαangiogenesisorallyvascularhypertensionABCG2Inhibitorinhibitorinhibit

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