Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H17N7O3 |
| Molecular Weight | 391.3834 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(N(CC(=O)NC3=NN=C(C=C3)C4=CC=CC=C4)C=N2)C(=O)N(C)C1=O
InChI
InChIKey=QTRXIFVSTWXRJJ-UHFFFAOYSA-N
InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27)
| Molecular Formula | C19H17N7O3 |
| Molecular Weight | 391.3834 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
ETC-159 (ETC-1922159) is an inhibitor of membrane-bound O-acyltransferase porcupine. Porcupine palmitoleates Wnt and this modification is essential for binding to chaperone WLS and Frizzled receptors and is therefore required for the activity of all Wnts. ETC-159 exerts antineoplastic properties both in vitro and in vivo due to inhibition of Wnt pathway. ETC-159 development has progressed to phase I clinical trial.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02521844 https://ascopubs.org/doi/abs/10.1200/JCO.2017.35.15_suppl.2584 https://oncologypro.esmo.org/Meeting-Resources/ESMO-Asia-2018-Congress/Phase-1-extension-study-of-ETC-159-an-oral-PORCN-inhibitor-administered-with-bone-protective-treatment-in-patients-with-advanced-solid-tumours
Phase I open-label, multi-centre study to determine safety, maximum tolerated dose, pharmacokinetics, pharmacodynamics (PD) of ETC-159 (1-30 mg) given orally in a 28d cycle.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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admin
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Edited
Sat Dec 16 11:19:44 GMT 2023
by
admin
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Sat Dec 16 11:19:44 GMT 2023
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5L854240DQ
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Validated (UNII)
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1638250-96-0
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86280523
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5L854240DQ
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ETC-159
Created by
admin on Sat Dec 16 11:19:44 GMT 2023 , Edited by admin on Sat Dec 16 11:19:44 GMT 2023
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PRIMARY | ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits .BETA.-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.IC50 value: 2.9 NM; Target: Wnt; 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 was approximately fourfold 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%. | ||
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C123830
Created by
admin on Sat Dec 16 11:19:44 GMT 2023 , Edited by admin on Sat Dec 16 11:19:44 GMT 2023
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
Originator: D3(Drug Product and Development), Biomedical Sciences Institute; Class: Antineoplastic; Mechanism of Action: PORCN protein inhibitor; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: Phase I for Solid tumours; Most Recent Event: 01 Oct 2015 Phase-I clinical trials in Solid tumours in USA (PO)
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