Repotrectinib (Synonyms: TPX-0005)

Name: Repotrectinib
Brand: MedChemExpress
SKU: HY-103022
Rating: 5.0 (4 reviews)

Cat. No.: HY-103022 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Repotrectinib Chemical Structure

CAS No. : 1802220-02-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 145	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 145	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 649	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Repotrectinib

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TrkA TrkB TrkC Trk

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

TrkA

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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

355.37

Formula

C₁₈H₁₈FN₅O₂

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (255 KB) HNMR (291 KB) LCMS (264 KB)

Handling Instructions (2659 KB)

References

[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

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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Repotrectinib (Synonyms: TPX-0005)

Customer Review

Repotrectinib Related Antibodies

4 Publications Citing Use of MCE Repotrectinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Trk Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Repotrectinib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Repotrectinib Related Classifications

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