GGTI2418;PTX 100|CAS 501010-06-6|DC Chemicals

Cas No.:	501010-06-6
Chemical Name:	Ggti-2418
Synonyms:	L-Leucine,N-[[(2S)-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-;(2S)-2-[[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino]-4-methylpentanoic acid;GGTI-2418;M67G28K74K;(S)-2-((S)-2-benzyl-4-((4-methyl-1H-imidazol-5-yl)methyl)-3-oxopiperazine-1-carboxamido)-4-methylpentanoic acid.;(S)-2-((S)-2-Benzyl-4-((5-methyl-1H-imidazol-4-yl)methyl)-3-oxopiperazine-1-carboxamido)-4-methylpentanoic acid;GGTI 2418;SC
SMILES:	O=C1[C@]([H])(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])N(C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])([H])N1C([H])([H])C1=C(C([H])([H])[H])N([H])C([H])=N1
Formula:	C₂₃H₃₁N₅O₄
M.Wt:	441.5233
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1].
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.
In Vitro:	GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM[1]. GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3[2]. Western Blot Analysis[2] Cell Line: HeLa cells Concentration: 10-15 μM Incubation Time: 16 hours Result: Delocalized FBXL2 and stabilized IP3R3.

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GGTI 2418