WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406424
CAS#: 251577-10-3 (free base)
Description: GGTI-2154 is a geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2154 results not only in halting the growth of aggressive breast tumors but actually in inducing the regression (54 +/- 3%) of all 19 tumors analyzed. The farnesyltransferase (FTase) inhibitor FTI-2148 induced an average of 87 +/- 3% regression in the 13 tumors analyzed. GGTase I, but not FTase, is inhibited in breast tumors after treatment with GGTI-2154, whereas in tumors from mice treated with FTI-2148, only FTase is inhibited. The processing of the geranylgeranylated proteins RhoA, Rap1, and R-Ras, but not the farnesylated proteins H-Ras and HDJ-2, is inhibited in tumors obtained from mice treated with GGTI-2154. GGTI-2154 and FTI-2148 suppress constitutively activated phospho-Erk1/2 and phospho-Akt, induce apoptosis, and induce differentiation toward ductolobular breast epithelium.
MedKoo Cat#: 406424
CAS#: 251577-10-3 (free base)
Chemical Formula: C24H28N4O3
Exact Mass: 420.21614
Molecular Weight: 420.50412
Elemental Analysis: C, 68.55; H, 6.71; N, 13.32; O, 11.41
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Related CAS #: 478908-50-8 (HCl) 251577-10-3 (free base)
Synonym: GGTI2154; GGTI 2154; GGTI-2154.
IUPAC/Chemical Name: L-Leucine, N-[[5-[(1H-imidazol-4-ylmethyl)amino]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-
InChi Key: GAJLKAVQYXFCRU-QFIPXVFZSA-N
InChi Code: InChI=1S/C24H28N4O3/c1-15(2)10-22(24(30)31)28-23(29)20-9-8-17(26-13-18-12-25-14-27-18)11-21(20)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)/t22-/m0/s1
SMILES Code: CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 420.50412 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Sun J, Ohkanda J, Coppola D, Yin H, Kothare M, Busciglio B, Hamilton AD, Sebti SM. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003 Dec 15;63(24):8922-9. PubMed PMID: 14695209.