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Fmoc-GGFG-Dxd

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Fmoc-GGFG-Dxd Basic information

Product Name:
Fmoc-GGFG-Dxd
Synonyms:
  • Glycinamide, N-[(9H-fluoren-9-ylmethoxy)carbonyl]glycylglycyl-L-phenylalanyl-N-[[2-[[(1S,9S)-9-ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]amino]-2-oxoethoxy]methyl]-
  • Fmoc-GGFG-Dxd
  • Exatecan-2-(aminomethoxy)acetamide-Gly-Phe-Gly-Gly-Fmoc
  • (S)-2-[2-[2-(Fmoc-amino)acetamido]acetamido]-N-[2-[[[2-[[(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-1,2,3,9,10,12,13,15-octahydrobenzo[de]pyrano[3’,4’:6,7]indolizino[1,2-b]quinolin-1-yl]amino]-2-oxoethoxy]methyl]amino]-2-oxoethyl]-3-phenylpropanamide
  • (S)-2-[2-[2-(Fmoc-amino)acetamido]acetamido]-N-[2-[[[2-[[(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-1,2,3,9,10,12,13,15-octahydrobenzo[de]pyrano[3’,4’:6,7]indolizino[1,2-b]quinolin-1-yl]amino]-2-oxoethoxy]methyl]amino]-2-oxoethyl]-3-phenylpropanamide
  • (9H-Fluoren-9-yl)methyl ((S)-10-benzyl-1-(((1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl)amino)-1,6,9,12,15-pentaoxo-3-oxa-5,8,11,14-tetraazahexadecan-16-yl)carbamate
CAS:
1599440-11-5
MF:
C57H55FN8O12
MW:
1063.09
Mol File:
1599440-11-5.mol
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Fmoc-GGFG-Dxd Chemical Properties

Density 
1.49±0.1 g/cm3(Predicted)
form 
Solid
pka
10.61±0.46(Predicted)
color 
Light yellow to yellow
InChIKey
DLIJZDSGDLLJKM-XWCAFGSDSA-N
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Fmoc-GGFG-Dxd Usage And Synthesis

Uses

Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D)[1].

Description

Fmoc-GGFG-Dxd, also known as N-((1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl)-2-hydroxyacetamide, is a brown powder. It is a hexacyclic chemical compound analogous to camptothecin with a triplet amino acid chain linked to a terminal Fmoc group. GGFG (glycyl-glycyl-phenylalanyl-glycine peptide could link exatecan derivative (DXd) through cysteine residues. DXd is highly membrane-permeable and exhibited strong bystander killing in-vitro co-culture of HER2 positive (KPL-4) and negative (MDA-MB-468) cells and in mice inoculated with a mixture of HER2 (+) and HER2 () cells.

IC 50

Traditional Cytotoxic Agents

storage

Powder -20℃ 2 years; In solvent -20℃ 1 month;

References

[1] Lingpei Kong, et al. Synthetic method for antibody-conjugated drug linker LND1067. CN113336823A.

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