2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. Cys-MC-GGFG-Dxd

Cys-MC-GGFG-Dxd is a cysteine-modified, cleavable ADC drug-linker conjugate. Cys-MC-GGFG-Dxd consists of a maleimidocaproyl-glycine-glycine-L-phenylalanine-glycine (MC-GGFG) linker and an Exatecan (HY-13631) derivative (DXd) (HY-13631D) payload. Cys-MC-GGFG-Dxd can be further conjugated to anti-HER2 IgG1κ antibody for the synthesis of antibody-drug conjugates (ADC), such as the breast cancer-targeting ADC compound Fam-trastuzumab deruxtecan-nxki (Enhertu).

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Cys-MC-GGFG-Dxd

Cys-MC-GGFG-Dxd Chemical Structure

CAS No. : 3025787-83-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Cys-MC-GGFG-Dxd:

Cys-MC-GGFG-Dxd Related Antibodies

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Description

Cys-MC-GGFG-Dxd is a cysteine-modified, cleavable ADC drug-linker conjugate. Cys-MC-GGFG-Dxd consists of a maleimidocaproyl-glycine-glycine-L-phenylalanine-glycine (MC-GGFG) linker and an Exatecan (HY-13631) derivative (DXd) (HY-13631D) payload. Cys-MC-GGFG-Dxd can be further conjugated to anti-HER2 IgG1κ antibody for the synthesis of antibody-drug conjugates (ADC), such as the breast cancer-targeting ADC compound Fam-trastuzumab deruxtecan-nxki (Enhertu)[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

In Vitro

The ADC conjugate related to Cys-MC-GGFG-DXd can also be generated via enzymatic hydrolysis of ADC in human liver lysosomes, human liver S9 fractions and H358 non-small cell lung cancer cells. The proportions of mass spectrometry peak areas of Cys-MC-GGFG-DXd reach 8.11%, 35.06% and 40.01% at 48 h in human liver lysosomes, 72 h in human liver S9 fractions and 96 h in tumor cells, respectively, making it the metabolite with the highest abundance besides the parent DXd[2].
Hydrolysis analysis results of Cys-MC-GGFG-Dxd show that Dxd is mainly released inside cells and then penetrates the cell membrane to enter the incubation medium; this mechanism serves as the critical basis for the "bystander effect"[2].

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

Cys-MC-GGFG-Dxd Related Antibodies
Molecular Weight

1155.21

Formula

C55H63FN10O15S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(CC(SC[C@H](N)C(O)=O)C1=O)N1CCCCCC(NCC(NCC(N[C@@H](CC2=CC=CC=C2)C(NCC(NCOCC(N[C@@H]3C4=C(CN5C6=CC7=C(COC([C@]7(O)CC)=O)C5=O)C6=NC8=CC(F)=C(C)C(CC3)=C48)=O)=O)=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (43.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8656 mL 4.3282 mL 8.6564 mL
5 mM 0.1731 mL 0.8656 mL 1.7313 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8656 mL 4.3282 mL 8.6564 mL 21.6411 mL
5 mM 0.1731 mL 0.8656 mL 1.7313 mL 4.3282 mL
10 mM 0.0866 mL 0.4328 mL 0.8656 mL 2.1641 mL
15 mM 0.0577 mL 0.2885 mL 0.5771 mL 1.4427 mL
20 mM 0.0433 mL 0.2164 mL 0.4328 mL 1.0821 mL
25 mM 0.0346 mL 0.1731 mL 0.3463 mL 0.8656 mL
30 mM 0.0289 mL 0.1443 mL 0.2885 mL 0.7214 mL
40 mM 0.0216 mL 0.1082 mL 0.2164 mL 0.5410 mL
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Cys-MC-GGFG-Dxd Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cys-MC-GGFG-Dxd3025787-83-8Drug-Linker Conjugates for ADCexatecan derivativeantibody-drug conjugatesmaleimidocaproyl-glycine-glycine-l-phenylalanine-glycinecysteine-conjugated linker-payload systemInhibitorinhibitorinhibit

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