Repotrectinib (Synonyms: TPX-0005)

Name: Repotrectinib
Brand: MedChemExpress
SKU: HY-103022
Rating: 5.0 (7 reviews)

製品番号: HY-103022 純度: 99.95%: Data Sheet SDS COA 取扱説明書
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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.

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CAS 番号 : 1802220-02-5

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$110	在庫あり	Estimated Time of Arrival: December 31
10 mg	$176	在庫あり	Estimated Time of Arrival: December 31
25 mg	$350	在庫あり	Estimated Time of Arrival: December 31
50 mg	$530	在庫あり	Estimated Time of Arrival: December 31
100 mg	$795	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Repotrectinib:

Repotrectinib (Standard) お問い合わせ

顧客検証

•bioRxiv. 2024 Feb 1.

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

: Repotrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]; Repotrectinib (1-1000 nM; 72 h) showed specific and significant activity in NTRK-Mono and NTRK-Pleo cell lines in vitro.

: Repotrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 16;16(1):5283. [Abstract]; Repotrectinib (2 mg/mL; i.g.; twice daily for 3 weeks) resulted in profound antitumor activity and complete tumor regression in mice bearing an NTRK-Mono allograft model.

: Repotrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]; Repotrectinib (15-75 mg/kg; twice daily for 24 d). Weight changes and survival analysis of Ba/F3 CD74-ROS1 G2032R luciferase mice.

: Repotrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2025 Jul 2;24(7):1005-1019. [Abstract]; Graph showed the number of resistant wells out of 480 and the distribution of kinase domain mutations among sequenced wells for Repotrectinib (5.6-28 nM; 28 d) in Ba/F3 CD74-ROS1 cells.

: Repotrectinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Mar 1;13(3):598-615. [Abstract]; Repotrectinib (15-75 mg/kg; i.g.; twice daily for 14 d) induced regression in the Ba/F3 CD74-ROS1 G2032R xenograft mice.

Trk Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

TrkA TrkB TrkC Trk

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

TrkA

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.7 1 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	0.66 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.8 1 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	0.7 1 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	2.2 1 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	0.88 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	0.66 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	208 1 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	0.98 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	0.7 1 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	4.8 1 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	1.14 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	0.88 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8 1 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]
BaF3	IC₅₀	1.39 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	0.98 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
KARPAS-299	IC₅₀	40 1 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]
BaF3	IC₅₀	1.61 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.14 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
NCI-H1373	IC₅₀	5000 1 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]
BaF3	IC₅₀	1.8 1 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	1.39 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.9 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
NCI-H1792	IC₅₀	1901 1 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]
BaF3	IC₅₀	1.61 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
NCI-H2122	IC₅₀	1936 1 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]
BaF3	IC₅₀	2.15 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.8 1 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 1 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]
NCI-H23	IC₅₀	4059 1 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 1 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]
BaF3	IC₅₀	1.9 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	3.32 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	10.67 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.59 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.8 1 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	10.83 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	12.28 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.4 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	15.66 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.75 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	158.95 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8 1 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]
BaF3	IC₅₀	17.04 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8.12 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	19.3 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	9.44 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.15 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	10.67 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.2 1 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	10.83 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	208 1 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	12.28 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	23.07 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	15.66 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	3.32 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	17.04 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.59 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	19.3 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.8 1 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	23.07 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.4 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
KARPAS-299	IC₅₀	40 1 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]
BaF3	IC₅₀	5.75 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	78.32 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	78.32 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	158.95 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8 1 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]
BaF3	IC₅₀	208 1 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	8.12 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
NCI-H1373	IC₅₀	5 3 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]
BaF3	IC₅₀	892.25 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	892.25 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	9.44 1 Compound: 4	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
NCI-H1792	IC₅₀	1901 1 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]
BaF3	IC₅₀	< 0.2 1 Compound: Repotrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition	[PMID: 36395392]
NCI-H2122	IC₅₀	1936 1 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-H358	IC₅₀	2500 1 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]
NCI-H23	IC₅₀	4059 1 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]
KARPAS-299	IC₅₀	40 1 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]
BaF3	IC₅₀	<0.2 1 Compound: Repotrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition	[PMID: 36395392]
NCI-H1373	IC₅₀	5000 1 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 1 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 1 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 1 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 1 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]

体外実験

Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC₅₀=1.26 nM) and ALK L1196M (IC₅₀=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC₅₀=1.04, 1.66, 5.3, and 6.96 nM, respectively)^[1].
Repotrectinib effectively overcomes this primary resistance (IC₅₀=100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC₅₀=13 nM) and the SRC substrate paxillin (IC₅₀=107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib^[1].

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

体内実験

Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts^[1].

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

臨床実験

分子量

355.37

分子式

C₁₈H₁₈FN₅O₂

CAS 番号

1802220-02-5

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (70.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2814 mL	1.4070 mL	2.8140 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.95%

Select Batch:

データシート (279 KB) SDS (393 KB)

COA (255 KB) RP-HPLC (261 KB) MS (68 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016

[2]. Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Repotrectinib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
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.

Keywords:

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

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Complete Stock Solution Preparation Table

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The molarity calculator equation

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