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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: 99.83%

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	Availability
1 mg	$34	In Stock
5 mg	$80	In Stock
10 mg	$122	In Stock
25 mg	$239	In Stock
50 mg	$355	In Stock
100 mg	$471	In Stock
1 mL x 10 mM (in DMSO)	$85	In Stock

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Purity:99.83%

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COA HPLC HNMR

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	TrkC:<2.5 nM, TrkA:0.6 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 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% Saline/PBS/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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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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