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Selitrectinib

Catalog No. T7435 CAS 2097002-61-2

Synonyms: 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)

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Selitrectinib, CAS 2097002-61-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 355.00
100 mg	In stock	$ 471.00
1 mL * 10 mM (in DMSO)	In stock	$ 85.00

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Purity: 99.83%

Purity: 99.55%

Purity: 98%

Purity: 95.49%

Biological Description

Chemical Properties

Storage & Solubility Information

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
Molecular Weight	380.42
Formula	C20H21FN6O
CAS No.	2097002-61-2

Storage

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

Solubility Information

DMSO: 62.5 mg/mL (164.29 mM)

References and Literature

1. Drilon A , Nagasubramanian R , Blake J F , et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors[J]. Cancer Discovery, 2017, 7(9):CD-17-0507.

Citations

1. Qin Q, Fu Q, Wang X, et al.Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.European Journal of Medicinal Chemistry.2023: 115291. 2. Qin Q, Guo Z, Lu S, et al.Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance.European Journal of Medicinal Chemistry.2023: 115953.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Pediatric Drug Library Orally Active Compound Library

Related Products

Related compounds with same targets

PF-06273340 LM22A-4 Amitriptyline hydrochloride TRK-IN-24 PF-06737007 ONO-7475 TrkA-IN-1 Ensartinib hydrochloride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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.

Keywords

Selitrectinib 2097002-61-2 Tyrosine Kinase/Adaptors Trk receptor LOXO195 Inhibitor LOXO 195 Tropomyosin related kinase receptor LOXO-195 Trk Receptor inhibit inhibitor

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