Description
GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.
Product information
CAS Number: 251577-10-3
Molecular Weight: 420.50
Formula: C24H28N4O3
Chemical Name: 2-[(4-{[(1H-imidazol-5-yl)methyl]amino}-2'-methyl-[1,1'-biphenyl]-2-yl)formamido]-4-methylpentanoic acid
Smiles: CC1=CC=CC=C1C1=CC=C(C=C1C(=O)NC(CC(C)C)C(O)=O)NCC1=CN=CN1
InChiKey: ROJBHAWUJUENON-UHFFFAOYSA-N
InChi: InChI=1S/C24H28N4O3/c1-15(2)10-22(24(30)31)28-23(29)21-11-17(26-13-18-12-25-14-27-18)8-9-20(21)19-7-5-4-6-16(19)3/h4-9,11-12,14-15,22,26H,10,13H2,1-3H3,(H,25,27)(H,28,29)(H,30,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM.
In Vivo:
GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice. GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%.
Products are for research use only. Not for human use.
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