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MC-Gly-Gly-Phe-Gly-GABA-Exatecan

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Catalog No. T87847Cas No. 1599439-52-7

MC-Gly-Gly-Phe-Gly-GABA-Exatecan, functioning both as an ADC linker agent and a topoisomerase inhibitor (Exatecan), displays cytotoxic and antitumor properties in vitro and in vivo [1] [2]. It specifically targets various antibodies and boasts an IC 50 of 22 μM.

MC-Gly-Gly-Phe-Gly-GABA-Exatecan

MC-Gly-Gly-Phe-Gly-GABA-Exatecan

😃Good
Catalog No. T87847Cas No. 1599439-52-7
MC-Gly-Gly-Phe-Gly-GABA-Exatecan, functioning both as an ADC linker agent and a topoisomerase inhibitor (Exatecan), displays cytotoxic and antitumor properties in vitro and in vivo [1] [2]. It specifically targets various antibodies and boasts an IC 50 of 22 μM.
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Product Introduction

Bioactivity
Description
MC-Gly-Gly-Phe-Gly-GABA-Exatecan, functioning both as an ADC linker agent and a topoisomerase inhibitor (Exatecan), displays cytotoxic and antitumor properties in vitro and in vivo [1] [2]. It specifically targets various antibodies and boasts an IC 50 of 22 μM.
In vitro
MC-Gly-Gly-Phe-Gly-GABA-Exatecan (0-10 μM) exhibits cytotoxicity by targeting antibodies CD30, CD33, CD70, and B7-H3 in the cell lines SR (CD30 positive), HL60 (CD33 positive), U251 (CD70 positive), and Calu-6 (B7-H3 positive) [2]. Cell Viability Assay [2] was conducted using SR, HL60, U251, and Calu-6 with a concentration range of 0-10 μM over 6 days, resulting in reduced cell viability.
In vivo
The compound MC-Gly-Gly-Phe-Gly-GABA-Exatecan, administered intravenously at 10 mg/kg once weekly for two weeks, demonstrates antitumor activity in A375 xenograft mice, resulting in inhibited tumor growth and induced tumor regression [2].
Chemical Properties
Molecular Weight1032.08
FormulaC53H58FN9O12
Cas No.1599439-52-7
SmilesN(C(CCCNC(CNC([C@H](CC1=CC=CC=C1)NC(CNC(CNC(CCCCCN2C(=O)C=CC2=O)=O)=O)=O)=O)=O)=O)[C@@H]3C4=C5C(C=6N(C5)C(=O)C7=C(C6)[C@](CC)(O)C(=O)OC7)=NC=8C4=C(CC3)C(C)=C(F)C8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

DrugLinkerConjugatesforADCDrugLinker Conjugates for ADC
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