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> VcMMAE [646502-53-6]

VcMMAE [646502-53-6]

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Referencia HY-15575-5mg

embalaje : 5mg

Marca : MedChemExpress

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Descripciòn

VcMMAE (mc-vc-PAB-MMAE) is a agent-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].

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

VcMMAE Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Peso molecular

1316.63

Fòrmula

C68H105N11O15
No. CAS
Appearance

Solid

Color

White to light yellow

SMILES

CC(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)(01)CCC2)=O)C)=O)=O)=O)C=C1)=O)=O)NC(CCCCCN4C(C=CC4=O)=O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

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

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 54 mg/mL (41.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (37.98 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (1.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% EtOH    90% Corn Oil

    Solubility: 2.5 mg/mL (1.90 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureza y Documentación
Referencias

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