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ETC-159

CAT: 0013-GTR19160464-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19160464-01Size:200 mg
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Description
ETC-159, also known as ETC-1922159, is a potent, selective and orally available PORCN inhibitor. ETC-159 blocks the secretion and activity of all Wnts. ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. Inhibition of Wnt signaling by PORCN inhibition holds promise as differentiation therapy in genetically defined human cancers. Enhanced sensitivity to Wnts is an emerging hallmark of a subset of cancers, defined in part by mutations regulating the abundance of their receptors. (In Vitro) :ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models driven by high Wnt signaling. ETC-159 is highly efficacious in molecularly defined colorectal cancers (CRCs) with R-spondin translocations (In Vivo) :ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately four fold higher (70 nM) . ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. ETC-159 exhibits good oral pharmacokinetics in mice allowing preclinical evaluation via oral administration. After a single oral dose of 5 mg/kg, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%.
CAS Number
1638250-96-0
Product Name Alternative
ETC-159 | ETC159 | ETC 159 | ETC-1922159
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 34 mg/m; L86.87 mM
Smiles
O=c1c2c (ncn2CC (=O) Nc2ccc (c3ccccc3) nn2) n (C) c (=O) n1C
Molecular Formula
C19H17N7O3
Molecular Weight
391.38
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1,3-dimethyl-7- ((6-phenylpyridazin-3-yl) glycyl) -3,4,5,7-tetrahydro-1H-purine-2,6-dione

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Alternative Products

CatalogName
BA9073-100ETC-159

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