646502-53-6 | MC-Val-Cit-PAB-MMAE

MMAE related articles:

• Total antibody quantification for MMAE-conjugated antibody-drug conjugates: impact of assay format and reagents.
• Therapeutic potential of an anti-CD79b antibody-drug conjugate, anti-CD79b-vc-MMAE, for the treatment of non-Hodgkin lymphoma

Description of VcMMAE

VcMMAE (also called as mc-vc-PAB-MMAE or MC-Val-Cit-PAB-MMAE) with CAS number 646502-53-6 is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

This compound is made by MMAE conjugated to MC-vc-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.

VcMMAE has Thiol Reactive groups which can react with antibody with Thiol(-SH).

VcMMAE is a MMAE derivative with valine-citrulline (Vc) linker. VcMMAE can be used to make antibody drug conjugate. VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc). Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself; instead, it is linked to a monoclonal antibody (MAB) which directs it to the cancer cells. In International Nonproprietary Names for MMAE-MAB-conjugates, the name vedotin refers to MMAE plus its linking structure to the antibody. It is a potent antimitotic drug derived from peptides occurring in marine shell-less mollusc Dolabella auricularia called dolastatins which show potent activity in preclinical studies, both in vitro and in vivo, against a range of lymphomas, leukemia and solid tumors. These drugs show potency of up to 200 times that of vinblastine, another antimitotic drug used for Hodgkin lymphoma as well as other types of cancer

Mechanism of VcMMAE

IC50 & Target is Auristatin. Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[1].

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[1].

Synonym of VcMMAE: VcMMAE; Vc-MMAE; MC-VC-PAB-MMAE; MMAE Vc linker, MMAE antibody conjugate

Appearance of VcMMAE: White to off-white solid powder
Purity of VcMMAE: >95%
Shipping Condition of VcMMAE: 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 of VcMMAE: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility of VcMMAE: Soluble in DMSO
Shelf Life of VcMMAE: >2 years if stored properly
Drug Formulation of VcMMAE: This drug may be formulated in DMSO
Stock Solution Storage of VcMMAE: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code of VcMMAE: 2934999001

References Articles of VcMMAE:

[1]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.

[2]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.

[3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.