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TRK-IN-24 (compound 10g) is a selective inhibitor of Trk receptors, effectively targeting TRKA, TRKC, and mutant forms TRKA G595R, TRKA G667C, and TRKA F589L, with corresponding IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM. It demonstrates antitumor activity in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models and inhibits the proliferation of Ba/F3 cells expressing single mutants SF, GK, and xDFG, with an IC50 range of 1.43-47.56 nM [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | Inquiry | 8-10 weeks | |
50 mg | Inquiry | 8-10 weeks |
Description | TRK-IN-24 (compound 10g) is a selective inhibitor of Trk receptors, effectively targeting TRKA, TRKC, and mutant forms TRKA G595R, TRKA G667C, and TRKA F589L, with corresponding IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM. It demonstrates antitumor activity in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models and inhibits the proliferation of Ba/F3 cells expressing single mutants SF, GK, and xDFG, with an IC50 range of 1.43-47.56 nM [1]. |
In vitro | TRK-IN-24 (Compound 10g) at concentrations ranging from 3.7 to 300 nM inhibits the phosphorylation of AKT, TRKA, PLCγ1, and ERK in Ba/F3 cells [1]. |
In vivo | TRK-IN-24 (compound 10g) administered at 50 mg/kg for 10-14 days resulted in 72% and 78% tumor regression in murine xenograft models of BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C, respectively [1]. |
Molecular Weight | 659.82 |
Formula | C39H45N7O3 |
Cas No. | 2937544-01-7 |
Storage | Shipping with blue ice. |
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