MedKoo Cat#: 207061 | Name: M8891
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Description:

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

M8891 is a potent and orally active methionine aminopeptidase 2 inhibitor with potential antiangiogenic and antineoplastic activities. Upon administration, MetAP2 inhibitor M8891 inhibits MetAP2 aminopeptidase activity and impairs protein synthesis, which may lead to a decrease in endothelial cell proliferation. Decreased proliferation of endothelial cells results in reductions of both angiogenesis and the growth and spread of solid tumors that are dependent on new blood vessel formation. MetAP2, a metallopeptidase, is involved in promoting protein synthesis and endothelial cell proliferation.

Chemical Structure

M8891
M8891
CAS#1464842-09-8

Theoretical Analysis

MedKoo Cat#: 207061

Name: M8891

CAS#: 1464842-09-8

Chemical Formula: C20H17F2N3O3

Exact Mass: 385.1238

Molecular Weight: 385.37

Elemental Analysis: C, 62.33; H, 4.45; F, 9.86; N, 10.90; O, 12.45

Price and Availability

Size Price Availability Quantity
5mg USD 850.00 2 Weeks
10mg USD 1,550.00 2 Weeks
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Related CAS #
No Data
Synonym
M8891; M-8891; M 8891;
IUPAC/Chemical Name
(S)-3-Hydroxy-1-(1H-indol-5-yl)-2-oxo-pyrrolidine-3-carboxylic Acid 3,5-Difluoro-benzylamide
InChi Key
WVGGJQVCOTYFPV-FQEVSTJZSA-N
InChi Code
InChI=1S/C20H17F2N3O3/c21-14-7-12(8-15(22)10-14)11-24-18(26)20(28)4-6-25(19(20)27)16-1-2-17-13(9-16)3-5-23-17/h1-3,5,7-10,23,28H,4,6,11H2,(H,24,26)/t20-/m0/s1
SMILES Code
O=C([C@]1(O)C(N(C2=CC3=C(NC=C3)C=C2)CC1)=O)NCC4=CC(F)=CC(F)=C4
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
Shelf Life
>3 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
Removal of N-terminal methionine by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. MetAP-2, one of the two cytoplasmic methionine aminopeptidases expressed in mammalian cells, has been identified as a target of the highly potent and irreversible inhibitor fumagillin, to which antiangiogenic and antitumoral properties have been ascribed.1−3 These and other findings rationalize the development of MetAP-2 inhibitors for cancer therapy. (Timo Heinrich: Journal of Medicinal Chemistry, Articles ASAP, Publication Date (Web):November 14, 2019)

Preparing Stock Solutions

The following data is based on the product molecular weight 385.37 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
1: Heinrich T, Seenisamy J, Becker F, Blume B, Bomke J, Dietz M, Eckert U, Friese-Hamim M, Gunera J, Hansen K, Leuthner B, Musil D, Pfalzgraf J, Rohdich F, Siegl C, Spuck D, Wegener A, Zenke FT. Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer. J Med Chem. 2019 Dec 3. doi: 10.1021/acs.jmedchem.9b01070. [Epub ahead of print] PubMed PMID: 31725285.