745017-94-1

  • Product Name:MonoMethylauristatin F
  • Molecular Formula:C39H65N5O8
  • Purity:99%
  • Molecular Weight:731.96
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Product Details:

CasNo: 745017-94-1

Molecular Formula: C39H65N5O8

Appearance: White to Off-White Solid

Delivery Time: 2 weeks after order

Throughput: 100KG/Month

Purity: 99%

Product Name: MonoMethylauristatin F
Synonyms: MMAF;MonoMethylauristatin F;MonoMethyl Auristatin F | MMAF;MMAF (MonoMethylauristatin F);Monomethyl auristatin phenylalanine;MONOMETHYLAURISTATIN F; MMAF; MONOMETHYL AURISTATIN PHENYLALANINE; 745017-94-1;(2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid;(2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid
CAS: 745017-94-1
MF: C39H65N5O8
MW: 731.96
EINECS:  
Product Categories: ADCs
Mol File: 745017-94-1.mol
MonoMethylauristatin F Structure
 
MonoMethylauristatin F Chemical Properties
Boiling point  896.8±65.0 °C(Predicted)
density  1.116±0.06 g/cm3(Predicted)
storage temp.  Sealed in dry,Room Temperature
solubility  Soluble in DMSO
form  A solid
pka 3.56±0.10(Predicted)
color  White to off-white
Stability: Hygroscopic
 
Safety Information
MSDS Information
 
 
MonoMethylauristatin F Usage And Synthesis
in vivo The maximum tolerated dose in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAF (Monomethylauristatin F) (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.
Description MMAF (Monomethylauristatin F) is an effective tubulin polymerization inhibitor, used as an anti-tumor drug. MMAF (Monomethylauristatin F) is widely used as the cytotoxic component of antibody-conjugated drugs (ADCs), such as Vorsetuzumab mafodotin and SGN-CD19A.
Uses Monomethyl Auristatin F is an antimicrotubule agent. A potent mitotic inhibitor.
Biological Activity MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.
Biotechnological Applications MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
in vitro MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC50s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay.

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