GGTI-297
- Product Name
- GGTI-297
- CAS No.
- 181045-83-0
- Chemical Name
- GGTI-297
- Synonyms
- GGTI-297;N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE, TFA;L-Leucine, N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-
- CBNumber
- CB7675276
- Molecular Formula
- C26H31N3O3S
- Formula Weight
- 465.61
- MOL File
- Mol file
GGTI-297 Property
- Boiling point:
- 709.0±60.0 °C(Predicted)
- Density
- 1.232±0.06 g/cm3(Predicted)
- pka
- 3.70±0.10(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P391Collect spillage. Hazardous to the aquatic environment
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 255373
- Product name
- GGTI 297
- Packaging
- 1mg
- Price
- $489
- Updated
- 2021/12/16
GGTI-297 Chemical Properties,Usage,Production
Description
GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).
Uses
GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras[1][2].
Definition
ChEBI: (2S)-2-[[[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)phenyl]-oxomethyl]amino]-4-methylpentanoic acid is a leucine derivative.
in vivo
GGTI-297 (70 mg/kg; ip; once a day; for 5-7 weeks) inhibits the growth in nude mice of A-549 and Calu-1 xenografts, both of which express K-Ras mutations[2].
| Animal Model: | Nude mice injected (8 week old) with A-549 or Calu-1 cells[2] |
| Dosage: | 70 mg/kg |
| Administration: | ip; once a day; for 5 weeks (A-549 cells) and 12 weeks (Calu-1) |
| Result: | Inhibited the growth in nude mice of A-549 and Calu-1 xenografts. |
References
[1] Y Qian, et al. Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. Bioorg Med Chem. 1998 Mar;6(3):293-9. DOI:10.1016/s0968-0896(97)10040-2
[2] J Sun, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-73. DOI:10.1038/sj.onc.1201656
GGTI-297 Preparation Products And Raw materials
Raw materials
Preparation Products
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