TPX-0046 (Enbezotinib) | RET inhibitor

Chemical Structure : TPX-0046

CAS No.: 2359649-81-1

TPX-0046 (Enbezotinib, TPX0046)

Catalog No.: PC-73416Not For Human Use, Lab Use Only.

TPX-0046 (Enbezotinib) 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.

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5 mg	$298	In stock
10 mg	$488	In stock
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Biological Activity

TPX-0046 (Enbezotinib) 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.

Physicochemical Properties

M.Wt	424.43
Formula	C21H21FN6O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
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

References

1. A.Drilon, et al. Annals of Oncology Volume 30, Supplement 5, October 2019, Pages v190-v191

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TPX-0046 (Enbezotinib, TPX0046)

Biological Activity

Physicochemical Properties

References

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