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TRK II-IN-1

Catalog No. T73033 CAS 2904690-41-9

TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. Additionally, this compound exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].

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TRK II-IN-1, CAS 2904690-41-9

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.

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Description	TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. Additionally, this compound exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].
Targets&IC50	TrkA:3.3 nM, TrkB:6.4 nM, TrkC:4.3 nM, FLT3:1.3 nM, RET:9.9 nM, VEGFR2:71.1 nM, TrkA G667C:9.4 nM
In vitro	TRK II-IN-1 (compound 12d) exhibited potent kinase inhibition activity, with over 90% inhibition of VEGFR2, RET, FLT3, and approximately 70% inhibition of Kit, CSF1R, DDR1, and DDR2 at 1 μM concentration [1]. At 72 hours, the compound effectively inhibited growth in Ba/F3 cell lines Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB, and Ba/F3-ETV6-TRKC, with respective IC50 values of 26.1, 44.7, and 15.7 nM [1]. It also hindered proliferation across a range of Ba/F3 cells harboring various types of TRK fusion proteins, including wild type and mutant forms, showing IC50 values between 2.6 and 143.3 nM [1]. Furthermore, TRK II-IN-1 induced apoptosis in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA G667C cells within a 48-hour exposure at concentrations spanning 0.4-500 nM [1], caused G0/G1 cell cycle arrest in the same cells over 24 hours [1], and dose-dependently suppressed phosphorylation of TRKA, TRKA G667C, AKT, ERK, and PLCγ1 after 6 hours of treatment within the range of 0.8-500 nM [1].

Molecular Weight	564.6
Formula	C29H31F3N8O
CAS No.	2904690-41-9

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

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Keywords

TRK II-IN-1 2904690-41-9 Tyrosine Kinase/Adaptors Trk receptor inhibitor inhibit

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