WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 207061
Description: 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.
MedKoo Cat#: 207061
Chemical Formula: C20H17F2N3O3
Exact Mass: 385.1238
Molecular Weight: 385.3708
Elemental Analysis: C, 62.33; H, 4.45; F, 9.86; N, 10.90; O, 12.45
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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
The following data is based on the product molecular weight 385.3708 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|
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.
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)