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
- Molecular Weight:
- 465.61
- MDL Number:
- MFCD02683590
- MOL File:
- Mol file
- MSDS File:
- SDS
- TDS File:
- TDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS09,GHS06 |
|---|---|
| Signal word | Danger |
| Hazard statements | H410-H301 |
| Precautionary statements | P273-P391-P501-P264-P270-P301+P310-P321-P330-P405-P501 |
GGTI-297 Chemical Properties, Uses, 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
GGTI-297 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8435 | 60 |
| Nantong Hi-Future Biotechnology Co., Ltd | +86-0513; 18051384581 | sales@chemhifuture.com | China | 3075 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49709 | 58 |
| Supplier | Advantage |
|---|---|
| BOC Sciences | 65 |
| EMMX Biotechnology LLC | 60 |
| Nantong Hi-Future Biotechnology Co., Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | 58 |
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