ChemicalBook--->CAS DataBase List--->1638250-96-0

1638250-96-0

1638250-96-0 Structure

1638250-96-0 Structure
IdentificationBack Directory
[Name]

ETC-159
[CAS]

1638250-96-0
[Synonyms]

ETC-159
CS-1584
ETC1922159
ETC-1922159
ETC 1922159
ETC 159;ETC159;ETC 1922159;ETC-1922159;ETC1922159
ETC-159;ETC 159;ETC159;ETC 1922159;ETC-1922159;ETC1922159
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide
7H-Purine-7-acetamide, 1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-
[Molecular Formula]

C19H17N7O3
[MOL File]

1638250-96-0.mol
[Molecular Weight]

391.38
Chemical PropertiesBack Directory
[density ]

1.47±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 33 mg/ml; DMSO: 33 mg/ml; DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml
[form ]

A crystalline solid
[pka]

11.28±0.70(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS06,GHS08,GHS09
[Signal word ]

Danger
[Hazard statements ]

H301-H371-H372-H411
[Precautionary statements ]

P501-P273-P260-P270-P264-P391-P308+P311-P301+P310+P330-P405
Hazard InformationBack Directory
[Uses]

1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide is a novel potent PORCN inhibitor that blocks the secretion and activity of all Wnts.
[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%[1].

[storage]

Store at -20°C
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