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VcMMAE Is An Antibody Drug with Anticancer Activity

VcMMAE Is An Antibody Drug with Anticancer Activity

English name：VcMMAE
CAS number：646502-53-6
Another name:
VcMMAE;MC-Val-Cit-PAB-MMAE;Maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl-monomethylauristatinE;4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanamido)benzyl((SChemicalbook)-1-(((S)-1-(((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-y;MC-VC-PAB-MMAE;MC-VC-PAB-MMAE,MC-Val-Cit-PAB-MMAE;maleimido-caproyl-val-Cit-PAB-MMAE;VeMMAE
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Products Description

 

English name：VcMMAE

CAS number：646502-53-6

Molecular formula: C68H105N11O15

Molecular weight: 1,316.63

EINECS No:

 

Related categories

Drug substance [for scientific research only]; pharmaceutical drug substances; medical raw materials; drug substances; standard raw materials; pharmaceutical raw materials; antibody conjugated drug intermediates; plant extraction; chemical reagents; chemical raw materials; ADCs; ADC; biological reagents; quality scientific research reagents

The Mol file, 646502-53-6.mol

structural formula:

 

Structural formula:

1 -

 

Nature of monomethylorerestatin E

Boiling point: 1347.6 ± 65.0 C (Predicted)

Density: 1.196±0.06g/cm3 (Predicted)

Storage conditions: Sealedindry, RoChemicalbookomTemperature

Solubility: Dissolve in DMSO, DCM, and DMF

Aciity coefficient (pK a): 13.29 ± 0.70 (Predicted)

Form: solid

Color: white to off-white

InChIKey:NLMBVBUNULOTNS-NNNQBTKHNA-N

 

Use and synthesis method of monomethylorerestatin E

 

Product description

VcMMAE (mc-vc-PAB-MMAE) is a biochemical reagent that is part of an antibody drug complex (drug-linChemicalbookkerconjugateforADC) with anticancer activity and is made of MMAE (a tubulin inhibitor) and Vc.

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VcMMAE (mc-vc-PAB-MMAE) is a drug linker conjugate of ADC, a lytic dipeptide, valine-citrulline (vc), through the use of the nucleolytic monomethyl ChemicalbookauristatinE (MMAE, tubulin inhibitor).

 

In vitro action

Monomethylotatin E (MMAE) is effectively released from SGN-35 in CD30 + cancer cells and exerts its cytotoxic activity against bystander cells due to its membrane permeability. MMChemicalbookAE Sensitize large intestine and pancreatic cancer cells to IR in a schedule and dose-dependent manner associated with mitotic arrest. Radiosensitization is evidenced by decreased survival of clone formation and increased DNA double-strand breaks after RT.

 

The role of the body

Monomethylic aurecatine E (MMAE) combined with IR causes delayed tumor growth, and ACPP-cRGD-MMAE targeted with IR produces more stable and significantly prolonged tumor regression in a xenograft model.

 

Bioactivity

VcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with a valine-citrulline (Vc) connector, is a antiChemicalbookbody-drugconjugate (ADC) with antitumor activity. MMAE is a synthetic antitumor agent that can be efficiently released from VcMMAE and exert cytotoxic activity in vitro.

 

Target spot

Auristatin

 

In vitro study

MonomethylauristatinE(MMAE)isefficientlyreleasedfromSGN-35withinCD30+cancercellsand,duetoitsmembranepermeability,isabletoexertcytotoxicactivityonbystandercells.MMAEsensitizedcolorectalandpancChemicalbookreaticcancercellstoIRinascheduleanddosedependentmannercorrelatingwithmitoticarrest.RadiosensitizationisevidencedbydecreasedclonogenicsurvivalandincreasedDNAdoublestrandbreaksinirradiatedcells.

 

In vivo research

Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models.

 

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