MMAF (Hydrochloride)

Modify Date: 2024-01-08 13:51:14

MMAF (Hydrochloride) Structure
MMAF (Hydrochloride) structure
Common Name MMAF (Hydrochloride)
CAS Number 1415246-68-2 Molecular Weight 768.42300
Density N/A Boiling Point N/A
Molecular Formula C39H66ClN5O8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MMAF (Hydrochloride)


MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.

 Names

Name ((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine hydrochloride
Synonym More Synonyms

 MMAF (Hydrochloride) Biological Activity

Description MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
Related Catalog
Target

IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

In Vitro MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].
In Vivo The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[1].
Cell Assay Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[1].
Animal Admin Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[1].
References

[1]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

 Chemical & Physical Properties

Molecular Formula C39H66ClN5O8
Molecular Weight 768.42300
Exact Mass 767.46000
PSA 166.61000
LogP 5.01620
Storage condition 2-8℃

 Synonyms

MMAF (Hydrochloride)