Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H27N3O4 |
| Molecular Weight | 409.4782 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)[C@H](O)C(=O)N[C@@H](C)C(=O)N[C@H]1C2=C(C=CC=C2)C3=C(C=CC=C3)N(C)C1=O
InChI
InChIKey=JURYTIUJMYPBNN-GKCIPKSASA-N
InChI=1S/C23H27N3O4/c1-13(2)20(27)22(29)24-14(3)21(28)25-19-17-11-6-5-9-15(17)16-10-7-8-12-18(16)26(4)23(19)30/h5-14,19-20,27H,1-4H3,(H,24,29)(H,25,28)/t14-,19-,20-/m0/s1
| Molecular Formula | C23H27N3O4 |
| Molecular Weight | 409.4782 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 14:58:29 GMT 2023
by
admin
on
Sat Dec 16 14:58:29 GMT 2023
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| Record UNII |
PX8XQ3H3RV
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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Systematic Name | English |
| Code System | Code | Type | Description | ||
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57327010
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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LY 900009
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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PRIMARY | MedKoo CAT NO.: 206715, CAS NO.: 209984-68-9Description: LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the .GAMMA.-secretase protein. LY900009 inhibited plasma levels of amyloid-.BETA. peptide in a dose-dependent manner with 80-90% inhibition observed in the 30- to 60-mg cohorts. LY900009 is an orally available GSI (A.BETA.: IC50= 10.912.1 nMNotch: IC50 = 14.1 nM) that was developed as a candidate therapeutic drug against AD (IDENTITY trial), which failed in phase III trials. (last updated: 4/18/2016). | ||
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LY-900009
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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PRIMARY | LY-900009 is a selective small-molecule inhibitor of .GAMMA.-secretase with IC50 value of 0.27nM.Notch signaling plays a critical role in stem cell function and is deragulated in different forms of cancer. .GAMMA.-secretase cleaves Notch receptor and regulates its signaling. LY-900009 is an oral notch inhibitor for the treatment of cancer but is now terminated in Phase I.The phase I study shows that LY900009 causes adverse events including diarrhea, vomiting, nausea, fatigue, anorexia, hypophosphatemia and rash at different grades. Treatment of 60mg LY900009 shows dose-limiting toxicities of fatigue and diarrhea respectively in 2 patients. The maximum tolerated dose (MTD) of LY900009 is identified at 30mg. And the elimination half-life is about 2-3 hrs. As a .GAMMA.-secretase inhibitor, LY900009 also decreases plasma levels of amyloid-.BETA. in a dose-dependent manner. | ||
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DTXSID701102553
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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PRIMARY | |||
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PX8XQ3H3RV
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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PRIMARY | |||
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209984-68-9
Created by
admin on Sat Dec 16 14:58:29 GMT 2023 , Edited by admin on Sat Dec 16 14:58:29 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
Originator: Eli Lilly; Class: Antineoplastic, Small molecule; Mechanism of Action: Amyloid precursor protein secretase inhibitor, Angiogenesis inhibitor, Apoptosis stimulant, Notch signalling pathway inhibitor; Orphan Drug Status: No; On Fast track: No; Highest Development Phase: Discontinued for Cancer; Most Recent Events: 17 Oct 2012 Discontinued - Phase-I for Cancer in USA (PO), 31 Aug 2012 Eli Lilly completes a phase I trial in Cancer in USA (NCT01158404), 20 Jul 2010 Phase-I clinical trials in Cancer in USA (PO)
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ACTIVE MOIETY |
Official Title: Phase 1 Study of a Notch Inhibitor in Patients With Advanced Cancer
Purpose: The objective of this phase 1 study is to evaluate the safety and tolerability of Notch Inhibitor in patients with advanced cancer. This study includes dose escalation and dose confirmation components.
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