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Selitrectinib

Name: Selitrectinib
Brand: TargetMol
SKU: T7435
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7435Cas No. 2097002-61-2

Alias LOXO-195

Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively).

Selitrectinib

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Purity: 99.97%

Catalog No. T7435Alias LOXO-195Cas No. 2097002-61-2

Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$122	In Stock	In Stock
25 mg	$239	In Stock	In Stock
50 mg	$355	In Stock	In Stock
100 mg	$471	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$85	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Purity:99.97%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively).
Targets&IC50	TrkA:0.6 nM , TrkC:<2.5 nM
In vivo	Selitrectinib (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.
Animal Research	Each cell line (2–5×10e6 cells) was injected subcutaneously into female nu/nu NCr mice age 7–9 weeks and allowed to grow to ~100–200 mm3 (efficacy) or ~ 500mm3 (PK-PD) prior to randomization by tumor size and treatment with each inhibitor by oral gavage.?For PK-PD analysis, animals were dosed for 3 days, followed by euthanasia, excision of tumors and collection of plasma.?Phospho-TRK levels in tumor lysates were determined by ELISA assay, while plasma inhibitor levels were determined by LC-MS/MS.?For efficacy analysis, animals were dosed by oral gavage, and body weight and tumor size were monitored at regular intervals.
Synonyms	LOXO-195

Chemical Properties

Molecular Weight	380.42
Formula	C₂₀H₂₁FN₆O
Cas No.	2097002-61-2
Smiles	[H][C@]12CCCN1c1ccn3ncc(C(=O)N[C@H](C)CCc4ncc(F)cc24)c3n1
Relative Density.	1.51 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 65 mg/mL (170.86 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6287 mL	13.1434 mL	26.2867 mL	131.4337 mL
5 mM	0.5257 mL	2.6287 mL	5.2573 mL	26.2867 mL
10 mM	0.2629 mL	1.3143 mL	2.6287 mL	13.1434 mL
20 mM	0.1314 mL	0.6572 mL	1.3143 mL	6.5717 mL
50 mM	0.0526 mL	0.2629 mL	0.5257 mL	2.6287 mL
100 mM	0.0263 mL	0.1314 mL	0.2629 mL	1.3143 mL

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In Vivo Formulation Calculator (Clear solution)

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

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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