M8891

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

MedKoo CAT#: 207061

CAS#: 1464842-09-8

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.


Chemical Structure

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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: 385.3708
Elemental Analysis: C, 62.33; H, 4.45; F, 9.86; N, 10.90; O, 12.45

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

Preparing Stock Solutions

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.

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

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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.



Additional Information

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)