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863971-24-8

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  • L-Valinamide, N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-N-methyl-L-valyl- N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenyl ethyl]amino]-1-methoxy-2-methyl-3-oxopropy

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  • L-Valinamide, N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-N-methyl-L-valyl- N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenyl ethyl]amino]-1-methoxy-2-methyl-3-oxopr

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  • L-Valinamide, N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-N-methyl-L-valyl- N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenyl ethyl]amino]-1-methoxy-2-methyl-3-oxopropy

    Cas No: 863971-24-8

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863971-24-8 Usage

General Description

McMMAE, also known as monomethyl auristatin E, is a powerful antineoplastic agent that inhibits cell division by blocking the polymerization of tubulin. It is mainly used as a cytotoxic component in antibody-drug conjugates (ADCs) for cancer treatment. However, due to its high toxicity, it should not be used on its own, but only linked to a specific antibody that directs it to the cancer cells. This ensures that healthy cells are not impacted, improving the efficiency and safety of cancer treatments. The most well-known ADC using McMMAE is Brentuximab vedotin, which is approved for the treatment of some types of lymphomas.

Check Digit Verification of cas no

The CAS Registry Mumber 863971-24-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,3,9,7 and 1 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 863971-24:
(8*8)+(7*6)+(6*3)+(5*9)+(4*7)+(3*1)+(2*2)+(1*4)=208
208 % 10 = 8
So 863971-24-8 is a valid CAS Registry Number.

863971-24-8SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name Maleimidocaproyl-monomethylauristatin E

1.2 Other means of identification

Product number -
Other names -

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:863971-24-8 SDS

863971-24-8Downstream Products

863971-24-8Relevant articles and documents

Antibody-drug conjugate using ionized CYS-linker-mmae as the potent payload shows optimal therapeutic safety

Fan, Shiyong,Li, Wei,Liu, Lianqi,Wang, Yanming,Xiao, Dian,Xie, Fei,Zhong, Wu,Zhou, Xinbo

, (2020/04/01)

Monomethyl auristatin E (MMAE) is the most popular and widely used cytotoxin in the development of antibody-drug conjugates (ADCs). However, current MMAE-based ADCs are all constructed using cleavable linkers, and this design concept still has insurmountable drawbacks. Their potential instabilities and lipophilic MMAE-induced “bystander effect” inevitably increase the toxicity to normal tissues. Herein, we overturn previous negative views of MMAE-based ADCs with non-cleavable linkers and propose using ionized L-Cysteine (Cys)-linker-MMAE as a novel payload, which can ingeniously enrich and enter tumor cells through receptor-mediated endocytosis of antibodies while its lower permeability helps to avoid further off-target toxicity. We demonstrate that Cys-linker-MMAE maintains high potency similar to free MMAE at the tubulin molecular level and can also be efficiently released in target cells. As a result, the preferred ADC (mil40-15) not only exhibits ideal plasma stability and maintains potent cytotoxicity as MMAE (IC50: 10?11 M), but also shows improved safety with lower bystander toxicity (IC50: 10?9 M), its maximum tolerated dose approaching the level of the naked antibody (160 mg/kg). This study indicated that Cys-linker-MMAE has the potential as a potent payload for ADCs, which is expected to provide novel strategies for the development of MMAE-based ADCs.

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