Bioactivity | 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]. |
In Vivo | GGTI-297(70 mg/kg;腹腔注射;每天一次;持续 5-7 周)可抑制裸鼠中 A-549 和 Calu-1 异种移植瘤的生长,这两种移植瘤均表达 K-Ras 突变[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 181045-83-0 |
Formula | C26H31N3O3S |
Molar Mass | 465.61 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [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. |