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Chemical Structure : TPX-0046 enantiomer
CAS No.: 2359650-19-2
Catalog No.: PC-49375Not For Human Use, Lab Use Only.
TPX-0046 (Enbezotinib) enantiomer is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $298 | In stock | |
| 10 mg | $478 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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TPX-0046 (Enbezotinib) enantiomer is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
TPX-0046 inhibited RET phosphorylation (IC50 < 10 nM) in tumor cell lines (LC2/ad, CCDC6-RET; TT, RET C634W) and Ba/F3 engineered RET models (WT, G810R).
TPX-0046 inhibited KIF5B-RET Ba/F3, LC2/ad, and TT cells with IC50 values of 1 nM in cell proliferation assays.
TPX-0046 potently inhibited Ba/F3 RET engineered cells with SFMs (e.g. G810C/R/S) with mean proliferation IC50 of 1-17 nM.
TPX-0046 demonstrated marked in vivo anti-tumor efficacy in RET-driven cell-derived and patient-derived xenograft tumor models, a single dose of 5 mg/kg TPX-0046 inhibited >80% of RET phosphorylation.
TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance.
| M.Wt | 424.436 | |
| Formula | C21H21FN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(13E,14E,15aS,18aR,5R)-35-fluoro-5-methyl-15,15a,16,17,18,18a-hexahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one |
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1. A.Drilon, et al. Annals of Oncology Volume 30, Supplement 5, October 2019, Pages v190-v191
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