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

Telatinib  (Synonyms: 替拉替尼; Bay 57-9352)

目录号: HY-10527 纯度: 99.60%
COA 产品使用指南

Telatinib是有口服活性的VEGFR2VEGFR3PDGFαc-Kit的小分子抑制剂,IC50值分别为6,4,15,1 nM。

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Telatinib Chemical Structure

Telatinib Chemical Structure

CAS No. : 332012-40-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880
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1 mg ¥320
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5 mg ¥800
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10 mg ¥1200
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25 mg ¥2400
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50 mg ¥3600
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100 mg ¥5000
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500 mg   询价  

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Customer Review

Other Forms of Telatinib:

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.

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 has low affinity for the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, or the Tie-2 receptor[2]. Telatinib is metabolized by various cytochrome P450 (CYP) isoforms including CYP3A4/3A5, CYP2C8, CYP2C9, and CYP2C19 as well as by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4), with the formation of the N-glucuronides of telatinib as the major biotransformation pathway in man. In vitro studies show telatinib to be a weak substrate of the adenosine triphosphate binding cassette (ABC) B1 (ABCB1) transporter[3]. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines. In addition, 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[4].

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

体内研究
(In Vivo)

Telatinib causes a significant decrease in endothelium-dependent and endothelium-independent vasodilation. VEGF inhibition by itself decreases NO synthesis, which promotes vasoconstriction, increases peripheral resistance, and therefore can induce an increase in blood pressure[1]. Telatinib (15 mg/kg) with doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[4].

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

Clinical Trial
分子量

409.83

Formula

C20H16ClN5O3

CAS 号
性状

固体

颜色

White to light yellow

中文名称

替拉替尼;特拉替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 46 mg/mL (112.24 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4400 mL 12.2002 mL 24.4004 mL
5 mM 0.4880 mL 2.4400 mL 4.8801 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.08 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.60%

参考文献
Kinase Assay
[4]

The vanadate (Vi)-sensitive ATPase activity of ABCG2 in the membrane of High Five insect cells is measured. Briefly, membrane (2 μg/0.06 mL) are incubated in ATPase assay buffer with or without 0.4 mM vanadate at 37°C for 5 min and then incubated with varying concentrations of telatinib at 37°C for 5 min. The ATPase reaction is started by the addition of 4 mM Mg-ATP. After incubating at 37°C for 10 min, the reactions are stopped by adding 0.05 mL of 10% SDS solution. The liberated inorganic phosphate is measured[4].

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

Animal Administration
[4]

Mice: The mice are randomized into four groups and treated with one of the following regimens: (a) vehicle (10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300) (q3d×6), (b) DOX (1.8 mg/kg, i.p., q3d×6), (c) telatinib dissolved in 10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300 (15 mg/kg, p.o., every 2nd and 3rd day; total 12 times), and (d) DOX (1.8 mg/kg, i.p., q3d×6) + telatinib (15 mg/kg, p.o., every 2nd and 3rd day, given 1 h before giving DOX; total 12 times). DOX for injection is prepared by dissolving in saline. Tumor volume is measured using calipers and body weights are recorded[4].

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

参考文献

Telatinib 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4400 mL 12.2002 mL 24.4004 mL 61.0009 mL
5 mM 0.4880 mL 2.4400 mL 4.8801 mL 12.2002 mL
10 mM 0.2440 mL 1.2200 mL 2.4400 mL 6.1001 mL
15 mM 0.1627 mL 0.8133 mL 1.6267 mL 4.0667 mL
20 mM 0.1220 mL 0.6100 mL 1.2200 mL 3.0500 mL
25 mM 0.0976 mL 0.4880 mL 0.9760 mL 2.4400 mL
30 mM 0.0813 mL 0.4067 mL 0.8133 mL 2.0334 mL
40 mM 0.0610 mL 0.3050 mL 0.6100 mL 1.5250 mL
50 mM 0.0488 mL 0.2440 mL 0.4880 mL 1.2200 mL
60 mM 0.0407 mL 0.2033 mL 0.4067 mL 1.0167 mL
80 mM 0.0305 mL 0.1525 mL 0.3050 mL 0.7625 mL
100 mM 0.0244 mL 0.1220 mL 0.2440 mL 0.6100 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.

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目录号:
HY-10527
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