WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206715
CAS#: 209984-68-9
Description: LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein. LY900009 inhibited plasma levels of amyloid-β peptide in a dose-dependent manner with 80-90% inhibition observed in the 30- to 60-mg cohorts. LY900009 is an orally available GSI (Aβ: IC50= 10.9−12.1 nM; Notch: IC50 = 14.1 nM) that was developed as a candidate therapeutic drug against AD (IDENTITY trial), which failed in phase III trials.
MedKoo Cat#: 206715
Name: LY900009
CAS#: 209984-68-9
Chemical Formula: C23H27N3O4
Exact Mass: 409.2002
Molecular Weight: 409.486
Elemental Analysis: C, 67.46; H, 6.65; N, 10.26; O, 15.63
Synonym: LY900009; LY-900009; LY 900009.
IUPAC/Chemical Name: (S)-2-hydroxy-3-methyl-N-((S)-1-(((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)amino)-1-oxopropan-2-yl)butanamide
InChi Key: JURYTIUJMYPBNN-GKCIPKSASA-N
InChi Code: 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
SMILES Code: CN1C([C@@H](NC([C@H](C)NC([C@@H](O)C(C)C)=O)=O)C2=C(C=CC=C2)C3=C1C=CC=C3)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein. |
| In vitro activity: | TBD |
| In vivo activity: | TBD |
The following data is based on the product molecular weight 409.486 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | TBD |
| In vitro protocol: | TBD |
| In vivo protocol: | TBD |
1: Pant S, Jones SF, Kurkjian CD, Infante JR, Moore KN, Burris HA, McMeekin DS,
Benhadji KA, Patel BK, Frenzel MJ, Kursar JD, Zamek-Gliszczynski MJ, Yuen ES,
Chan EM, Bendell JC. A first-in-human phase I study of the oral Notch inhibitor,
LY900009, in patients with advanced cancer. Eur J Cancer. 2016 Mar;56:1-9. doi:
10.1016/j.ejca.2015.11.021. Epub 2016 Jan 19. PubMed PMID: 26798966.
