2. Protein Tyrosine Kinase/RTK Neuronal Signaling
  3. ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK)
  4. Repotrectinib

Repotrectinib  (Synonyms: 瑞普替尼; TPX-0005)

目录号: HY-103022 纯度: 99.90%
COA 产品使用指南

摩尔计算器

Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC50=0.07 nM) 和 TRK (对 TRKA/B/C 的 IC50=0.83/0.05/0.1 nM) 抑制剂。Repotrectinib 有效抑制 WT ALK (IC50=1.01 nM)。Repotrectinib 具有抗癌活性。

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Repotrectinib Chemical Structure

Repotrectinib Chemical Structure

CAS No. : 1802220-02-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥860
In-stock
1 mg ￥363
In-stock
5 mg ￥800
In-stock
10 mg ￥1200
In-stock
25 mg ￥2400
In-stock
50 mg ￥3600
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* Please select Quantity before adding items.

Customer Review

Repotrectinib 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

查看所有亚型
TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity[1][2].

IC50 & Target

TrkA

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
0.7 nM
Compound: TPX-0005
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
[PMID: 34253025]
BaF3 IC50
1.8 nM
Compound: TPX-0005
Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
[PMID: 34253025]
BaF3 IC50
2.2 nM
Compound: TPX-0005
Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
[PMID: 34253025]
BaF3 IC50
208 nM
Compound: TPX-0005
Antiproliferative activity against EML4-ALK-L1196M/G1202R mutated mouse BaF3 cells assessed as cell growth inhibition by CCK-8 assay
Antiproliferative activity against EML4-ALK-L1196M/G1202R mutated mouse BaF3 cells assessed as cell growth inhibition by CCK-8 assay
[PMID: 37127101]
BaF3 IC50
4.8 nM
Compound: TPX-0005
Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
[PMID: 34253025]
BaF3 IC50
8 nM
Compound: TPX-0005
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
[PMID: 34253025]
KARPAS-299 IC50
40 nM
Compound: TPX-0005
Antiproliferative activity against human KARPAS-299 cells assessed as cell growth inhibition by CCK-8 assay
Antiproliferative activity against human KARPAS-299 cells assessed as cell growth inhibition by CCK-8 assay
[PMID: 37127101]
NCI-H1373 IC50
5000 nM
Compound: 1
Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
[PMID: 34676026]
NCI-H1792 IC50
1901 nM
Compound: 1
Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
[PMID: 34676026]
NCI-H2122 IC50
1936 nM
Compound: 1
Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
[PMID: 34676026]
NCI-H23 IC50
4059 nM
Compound: 1
Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
[PMID: 34676026]
NCI-H358 IC50
2500 nM
Compound: 1
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay
[PMID: 34676026]
体外研究
(In Vitro)

Repotrectinib (TPX-0005) 抑制突变体 ALK，包括 ALK G1202R (IC50=1.26 nM) 和 ALK L1196M (IC50=1.08 nM)。Repotrectinib 还抑制多种其他激酶，包括 JAK2、LYN、Src 和 FAK (IC50=1.04、1.66、5.3 和 6.96 nM)[1]。
Repotrectinib 有效地克服了这种原发性耐药性 (细胞增殖试验中IC50=100 nM)，强烈抑制 EML4-ALK 的磷酸化 (IC50=13) nM) 和 SRC 底物桩蛋白 (IC50=107 nM)。Repotrectinib 在伤口愈合试验中抑制 H2228 细胞迁移，其活性与 saracatinib相似[1]。

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

Repotrectinib 相关抗体:
体内研究
(In Vivo)

Repotrectinib (TPX-0005) 在 ALK WT 和 ALK G1202R 异种移植物中有效抑制体内肿瘤生长[1]。

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

355.37

Formula

C18H18FN5O2
CAS 号
性状

固体

颜色

White to off-white

中文名称

瑞普替尼
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (70.35 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 2.8140 mL 14.0698 mL 28.1397 mL
5 mM 0.5628 mL 2.8140 mL 5.6279 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

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: ≥ 2.5 mg/mL (7.03 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.03 mM); 澄清溶液

    此方案可获得 ≥ 2.5 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 25.0 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

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: 99.90%

COA (199 KB) HNMR (260 KB) LCMS (263 KB)

产品使用指南 (1538 KB)
参考文献

Repotrectinib 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 2.8140 mL 14.0698 mL 28.1397 mL 70.3492 mL
5 mM 0.5628 mL 2.8140 mL 5.6279 mL 14.0698 mL
10 mM 0.2814 mL 1.4070 mL 2.8140 mL 7.0349 mL
15 mM 0.1876 mL 0.9380 mL 1.8760 mL 4.6899 mL
20 mM 0.1407 mL 0.7035 mL 1.4070 mL 3.5175 mL
25 mM 0.1126 mL 0.5628 mL 1.1256 mL 2.8140 mL
30 mM 0.0938 mL 0.4690 mL 0.9380 mL 2.3450 mL
40 mM 0.0703 mL 0.3517 mL 0.7035 mL 1.7587 mL
50 mM 0.0563 mL 0.2814 mL 0.5628 mL 1.4070 mL
60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1725 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:

Repotrectinib1802220-02-5TPX-0005瑞普替尼TPX0005TPX 0005ROS KinaseTrk ReceptorAnaplastic lymphoma kinase (ALK)Tropomyosin related kinase receptor Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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