[CAS NO. 646502-53-6]  VcMMAE

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PRODUCTS SPECIFICATIONS [646502-53-6]

Store
Catalog
HY-15575
Brand
MCE
CAS
646502-53-6

DESCRIPTION [646502-53-6]

Overview

MDLMFCD25372036
Molecular Weight1316.63
Molecular FormulaC68H105N11O15
SMILESCC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(COC(N(C)[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N2[C@@]([C@H](OC)[C@@H](C)C(N[C@H](C)[C@@H](O)C3=CC=CC=C3)=O)([H])CCC2)=O)C)=O)=O)=O)C=C1)=O)=O)NC(CCCCCN4C(C=CC4=O)=O)=O

For research use only. We do not sell to patients.


Summary

VcMMAE (mc-vc-PAB-MMAE) 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).


IC50 & Target

Auristatin


In Vitro

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 [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

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 [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, sealed storage, away from moisture and light

* The compound is unstable in solutions, freshly prepared is recommended.


Solvent & Solubility

In Vitro:

DMSO : ≥ 54 mg/mL ( 41.01 mM )

H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7595 mL 3.7976 mL 7.5951 mL
5 mM 0.1519 mL 0.7595 mL 1.5190 mL
10 mM 0.0760 mL 0.3798 mL 0.7595 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl [3] .