MedKoo Cat#: 206715 | Name: LY900009
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

LY900009
LY900009
CAS#209984-68-9

Theoretical Analysis

MedKoo Cat#: 206715

Name: LY900009

CAS#: 209984-68-9

Chemical Formula: C23H27N3O4

Exact Mass: 409.2002

Molecular Weight: 409.49

Elemental Analysis: C, 67.46; H, 6.65; N, 10.26; O, 15.63

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,150.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 2,950.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 5,850.00 2 Weeks
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Related CAS #
No Data
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
More Info
Product Data
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

Preparing Stock Solutions

The following data is based on the product molecular weight 409.49 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.

Recalculate based on batch purity %
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.