Tepotinib (Synonyms: 特泊替尼; EMD-1214063)

目录号: HY-14721 纯度: 99.94%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Tepotinib (EMD-1214063) 是一种具有口服活性的、高度选择性，可逆的，ATP-竞争性的 c-Met 抑制剂，IC₅₀ 为 3 nM，对 c-Met 的选择性比 IRAK4，TrkA，Axl，IRAK1 和 Mer 高 200 倍以上。Tepotinib 抑制 c-Met 磷酸化，诱导自噬 (autophagy)。Tepotinib 具有抗肿瘤作用。

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Tepotinib Chemical Structure

CAS No. : 1100598-32-0

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可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥975	In-stock
5 mg	￥900	In-stock
10 mg	￥1600	In-stock
50 mg	￥4092	In-stock
100 mg	￥5500	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Tepotinib:

Tepotinib (Standard) In-stock
Tepotinib hydrochloride 询价

MCE 顾客使用本产品发表的 5 篇科研文献

: Tepotinib purchased from MCE. Usage Cited in: Gene Expr. 2018 May 18;18(2):135-147. [Abstract]; Western blot for Myc-tag shows decrease in Myc-tag levels at 8 weeks of EMD1214063 treatment only. GAPDH shows comparable loading in all lanes.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC₅₀ of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects^[1]^[2]^[3].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	12 nM Compound: 22	Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay	[PMID: 25736998]
AGS	IC₅₀	1448 nM Compound: 3; T6121	Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	1.5 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	10 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	2.5 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	2385 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	3055 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	36.6 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	46.7 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	8.8 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
Hs746T	IC₅₀	4.5 nM Compound: 3; T6121	Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay	[PMID: 36355693]
SNU-16	IC₅₀	363 nM Compound: 3; T6121	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]

体外研究
(In Vitro)

Tepotinib 抑制 IRAK4、TrkA、Axl、IRAK1、Mer 和 TrkA，IC₅₀ 分别为 615、1017、1566、2037、2272 和 5716 nM^[1]。
Tepotinib 抑制 A549 细胞中 HGF 诱导的 c-Met 磷酸化，平均 IC₅₀ 为 6 nM^[1]。
Tepotinib (0.01 nM-30 μM) 可在体外抑制肿瘤细胞增殖和迁移^[1]。

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

Cell Viability Assay^[1]

Cell Line:	MKN-45 gastric cancer cells
Concentration:	0.01 nM, 0.03 nM, 0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM and 30 μM
Incubation Time:	72 hours
Result:	Considerably inhibited the viability of MKN-45 cells with IC₅₀ values of less than 1 nM.

体内研究
(In Vivo)

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

Animal Model:	CD-1 or BALB/C nude mice bearing human cancer cell lines KP-4, or EBC-1^[1]
Dosage:	6 and 15 mg/kg for mice bearing NSCLC EBC-1; 25, 50 and 200 mg/kg for mice bearing pancreatic carcinoma cell line KP-4.
Administration:	Injected daily; for 14-18 days
Result:	Daily administration of 5 or 15 mg/kg to EBC-1 tumor-bearing mice resulted in effective inhibition or complete tumor regression, respectively. Induced dose-dependent tumor growth inhibition in mice bearing human pancreatic carcinoma KP-4 tumors.

分子量

492.57

Formula

C₂₉H₂₈N₆O₂

CAS 号

1100598-32-0

性状

固体

颜色

White to light yellow

中文名称

特泊替尼；特普替尼

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 8.75 mg/mL (17.76 mM; 超声助溶 (<60°C); 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	2.0302 mL	10.1508 mL	20.3017 mL
5 mM	0.4060 mL	2.0302 mL	4.0603 mL
10 mM	0.2030 mL	1.0151 mL	2.0302 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。-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)

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)

动物实验：

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.62 mg/mL (1.26 mM); 澄清溶液

此方案可获得 ≥ 0.62 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.62 mg/mL (1.26 mM); 澄清溶液

此方案可获得 ≥ 0.62 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.62 mg/mL (1.26 mM); 澄清溶液

此方案可获得 ≥ 0.62 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。
以 1 mL 工作液为例，取 100 μL 6.2 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

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

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: 99.94%

选择批次：

Data Sheet (626 KB) SDS (393 KB)

COA (281 KB) HNMR (273 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Bladt F, et al. EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 2013, 19(11), 2941-2951. [Content Brief]

[2]. Zhan N, et al. The Effect of Selective c-MET Inhibitor on Hepatocellular Carcinoma in the MET-Active, β-Catenin-Mutated Mouse Model. Gene Expr. 2018 May 18;18(2):135-147. [Content Brief]

[3]. A. Naing, et al. IS4-1 - A Phase I Dose-Escalation Study of emd 1214063, an Oral Selective CMET Inhibitor, in Patients with Advanced Solid Tumors. Annals of Oncology. Volume 23, Supplement 11, October 2012, Page xi21.

Tepotinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0302 mL	10.1508 mL	20.3017 mL	50.7542 mL
	5 mM	0.4060 mL	2.0302 mL	4.0603 mL	10.1508 mL
	10 mM	0.2030 mL	1.0151 mL	2.0302 mL	5.0754 mL
	15 mM	0.1353 mL	0.6767 mL	1.3534 mL	3.3836 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:

Tepotinib1100598-32-0EMD-1214063特泊替尼特普替尼EMD1214063EMD 1214063c-Met/HGFRAutophagyInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Tepotinib (Synonyms: 特泊替尼; EMD-1214063)

Customer Review

Other Forms of Tepotinib:

MCE 顾客使用本产品发表的 5 篇科研文献