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Chemical Structure : TY-2136
Catalog No.: PC-21571Not For Human Use, Lab Use Only.
TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.
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TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.
TY-2136 shows similar potency to TPX-0005 inhibiting ROS1 G2032R mutant activity, confers significantly stronger potency than LOXO-101 inhibiting TRKA activity with G595R substitution.
TY-2136b is similar potent as TPX-0005 inhibiting cell proliferation of the Ba/F3 strain expressing mutant ROS1 bearing G2032R mutation, a major resistance mutation.
TY-2136b also shows potent inhibition towards ROS1, ERK and AKT phosphorylation and downstream signaling in Ba/F3-CD74-ROS1-G2032R cells.
TY-2136b is better than TPX-0005 and LOXO-195 against TRKA G595R/F589L dual mutations in vitro.
TY-2136b shows dose-dependent anti-tumor effect at the dose of 5, 10, and 20 mg/kg, bid, in xenograft tumor models carrying ROS1 G2032R and TRKA G595R mutation, and is more effective than Crizotinib and LOXO-101.
| M.Wt | 390.37 | |
| Formula | C18H17F3N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Chengshan Niu, et al. Cancer Res (2023) 83 (7_Supplement): 3400.
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