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Trk-IN-20

Catalog No. T61551 CAS 2460924-63-2

Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1].

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Trk-IN-20, CAS 2460924-63-2

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1].
In vitro	Trk-IN-20 (compound 7mb), identified as a potent inhibitor of Trk kinases, demonstrates significant efficacy against Larotrectinib-resistant colon cancer cells harboring NTRK1-G667C or NTRK3-G696A mutations, with IC50 values of 0.031 and 0.018 µM, respectively. Additionally, it effectively suppresses the activation of Trk and its downstream proteins in BaF3 murine cells expressing oncogenic NTRK fusions (CD74-NTRK1, ETV6-NTRK2, and ETV6-NTRK3), showcasing IC50s ranging from 9 to 22 nM. Further evaluations reveal that Trk-IN-20 binds tightly to the ATP-binding sites of TrkA/B/C with low nanomolar affinity (Kd values between 1.6 and 4.9 nM) and inhibits downstream signaling molecules such as ERK, AKT, and PLC-γ1 in a concentration-dependent manner, while also inducing partial degradation of Trk proteins in certain cell lines. These findings, supported by Western Blot analysis, underscore Trk-IN-20's potential as a targeted therapy for diverse human cancers with NTRK gene fusions.
In vivo	Trk-IN-20 (compound 7mb), administered orally at a dosage of 10 mg/kg, exhibits a short half-life of 1.39 hours and low oral bioavailability of 8.79% in rats. This indicates a rapid clearance from the body and limited absorption when administrated by mouth. The pharmacokinetic data, including area under the curve (AUC), maximum concentration (Cmax), half-life (T1/2), and clearance rate (CL) for both intravenous (i.v.) and oral (p.o.) routes, suggest a significant difference in the drug's absorption and distribution in the animal model [1].

Molecular Weight	376.4
Formula	C22H18F2N4
CAS No.	2460924-63-2

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

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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

Trk-IN-20 2460924-63-2 inhibitor inhibit

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