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180977-34-8

180977-34-8 structure
180977-34-8 structure
  • Name: FTI-277 (hydrochloride)
  • Chemical Name: 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride
  • CAS Number: 180977-34-8
  • Molecular Formula: C22H30ClN3O3S2
  • Molecular Weight: 484.07500
  • Catalog: Biochemical Inhibitor Metabolism Transferase inhibitor
  • Create Date: 2018-06-20 18:32:59
  • Modify Date: 2024-01-06 12:28:49
  • FTI-277 Hcl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.IC50 value:Target: FTase inhibitorin vitro: Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].in vivo: FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].

Name 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride
Synonyms FTI 277 HCl
FTI-277 (hydrochloride)
Description FTI-277 Hcl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.IC50 value:Target: FTase inhibitorin vitro: Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].in vivo: FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].
Related Catalog
References

[1]. Cohen-Jonathan E, et al. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11.

[2]. Nakazawa H, et al. Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle. PLoS One. 2015 Jan 16;10(1):e0116633.

[3]. Virtanen SS, et al. Inhibition of GGTase-I and FTase disrupts cytoskeletal organization of human PC-3 prostate cancer cells. Cell Biol Int. 2010 Aug;34(8):815-26.

Molecular Formula C22H30ClN3O3S2
Molecular Weight 484.07500
Exact Mass 483.14200
PSA 157.55000
LogP 5.01330
Appearance amorphous semi-solid
Storage condition −20°C
Water Solubility H2O: soluble
Hazard Codes Xi
Risk Phrases 36/37/38
Safety Phrases 26-36
WGK Germany 3