Shopping Cart

Remove All

Your shopping cart is currently empty

Entrectinib

Select Batch

Purity:99.61%

Resource Download

COA HPLC HNMR

Entrectinib

Catalog No. T3678Cas No. 1108743-60-7

Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
2 mg	$35	In Stock
5 mg	$54	In Stock
10 mg	$81	In Stock
25 mg	$113	In Stock
50 mg	$171	In Stock
100 mg	$297	In Stock
500 mg	$728	In Stock
1 mL x 10 mM (in DMSO)	$63	In Stock

Bulk & Custom

Add to Cart

Questions

Related Compound Libraries of "Entrectinib"

Product Introduction

Bioactivity

Description	Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
In vitro	Entrectinib effectively inhibits ALK‐dependent signaling and specificity blocks proliferation of ALK-dependent cell lines. Entrectinib also significantly inhibits cell growth of the NCI‐H2228 cell line bearing the EML4-ALK rearrangement.
In vivo	In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]
Cell Research	NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol[2].
Alias	RXDX-101, NMS-E628

Chemical Properties

Molecular Weight	560.64
Formula	C31H34F2N6O2
Cas No.	1108743-60-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 67 mg/mL(119.5 mM)

DMSO: 50 mg/mL (89.18 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

5% DMSO+95% Saline: 5 mg/mL (8.92 mM, precipitation)

Solution Preparation Table

Ethanol/5% DMSO+95% Saline

	1mg	5mg	10mg	50mg
1 mM	1.7837 mL	8.9184 mL	17.8368 mL	89.1838 mL
5 mM	0.3567 mL	1.7837 mL	3.5674 mL	17.8368 mL

Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.1784 mL	0.8918 mL	1.7837 mL	8.9184 mL
20 mM	0.0892 mL	0.4459 mL	0.8918 mL	4.4592 mL
50 mM	0.0357 mL	0.1784 mL	0.3567 mL	1.7837 mL
100 mM	0.0178 mL	0.0892 mL	0.1784 mL	0.8918 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc