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GGTI-2418

Basic information Safety Supplier Related

GGTI-2418 Basic information

Product Name:
GGTI-2418
Synonyms:
  • GGTI-2418
  • (S)-3-benzyl-1-((4-methyl-1-trityl-1H-imidazol-5-yl)methyl)piperazin-2-one
  • GGTI2418;PTX 100
  • GGTI 2418 (GGTI2418
  • L-Leucine, N-[[(2S)-4-[(4-methyl-1H-imidazol-5-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-
  • L-Leucine, N-[[(2S)-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-
  • (S)-2-((S)-2-Benzyl-4-((5-methyl-1H-imidazol-4-yl)methyl)-3-oxopiperazine-1-carboxamido)-4-methylpentanoic acid
  • PTX-100 (GGTI-2418)
CAS:
501010-06-6
MF:
C23H31N5O4
MW:
441.52
Mol File:
501010-06-6.mol
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GGTI-2418 Chemical Properties

Boiling point:
807.5±65.0 °C(Predicted)
Density 
1.270±0.06 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
DMSO:125.0(Max Conc. mg/mL);283.11(Max Conc. mM)
form 
A crystalline solid
pka
4.30±0.21(Predicted)
color 
Light yellow to yellow
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GGTI-2418 Usage And Synthesis

Uses

GGTI 2418 is a geranylgeranyltransferase I inhibitor.

in vivo

GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts[1].
GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice[1].
GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo[1].

Animal Model:Nude mice implanted with MDA-MB-231 breast cancer tumors[1]
Dosage:100 mg/kg daily or 200 mg/kg every third day
Administration:Injected intraperitoneally; 15 days
Result:Inhibited the growth of breast tumor xenografts.
Animal Model:ErbB2 transgenic mice[1]
Dosage:100 mg/kg/day
Administration:Subcutaneously; 5 days
Result:Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

GGTI-2418Supplier

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