Synonym
GGTI2417; GGTI-2417; GGTI 2417
IUPAC/Chemical Name
methyl ((S)-2-benzyl-4-((5-methyl-1H-imidazol-4-yl)methyl)-3-oxopiperazine-1-carbonyl)-L-leucinate
InChi Key
DWKYALWDWAYMTB-FPOVZHCZSA-N
InChi Code
InChI=1S/C24H33N5O4/c1-16(2)12-19(23(31)33-4)27-24(32)29-11-10-28(14-20-17(3)25-15-26-20)22(30)21(29)13-18-8-6-5-7-9-18/h5-9,15-16,19,21H,10-14H2,1-4H3,(H,25,26)(H,27,32)/t19-,21-/m0/s1
SMILES Code
CC(C)C[C@@H](C(OC)=O)NC(N1[C@@H](CC2=CC=CC=C2)C(N(CC3=C(C)NC=N3)CC1)=O)=O
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
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
More Info
Geranylgeranyltransferase I inhibitors (GGTIs) are presently undergoing advanced preclinical studies and have been shown to disrupt oncogenic and tumor survival pathways, to inhibit anchorage-dependent and -independent growth, and to induce apoptosis.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
455.56
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: Kazi A, Carie A, Blaskovich MA, Bucher C, Thai V, Moulder S, Peng H, Carrico
D, Pusateri E, Pledger WJ, Berndt N, Hamilton A, Sebti SM. Blockade of protein
geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and
accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol
Cell Biol. 2009 Apr;29(8):2254-63. doi: 10.1128/MCB.01029-08. Epub 2009 Feb 9.
PubMed PMID: 19204084; PubMed Central PMCID: PMC2663293.
2: Falsetti SC, Wang DA, Peng H, Carrico D, Cox AD, Der CJ, Hamilton AD, Sebti
SM. Geranylgeranyltransferase I inhibitors target RalB to inhibit
anchorage-dependent growth and induce apoptosis and RalA to inhibit
anchorage-independent growth. Mol Cell Biol. 2007 Nov;27(22):8003-14. Epub 2007
Sep 17. PubMed PMID: 17875936; PubMed Central PMCID: PMC2169159.
