[CAS NO. 180977-34-8]  FTI 277 HCl

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PRODUCTS SPECIFICATIONS [180977-34-8]

Store
Catalog
SLK-S7465
Brand
Selleck
CAS
180977-34-8

DESCRIPTION [180977-34-8]

Overview

MDLMFCD28385886
Molecular Weight484.07
Molecular FormulaC22H30ClN3O3S2
SMILESCSCC[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.0658 mL10.3291 mL20.6582 mL
5 mM0.4132 mL2.0658 mL4.1316 mL
10 mM0.2066 mL1.0329 mL2.0658 mL
50 mM0.0413 mL0.2066 mL0.4132 mL

Description

FTI 277 HCl is a potent and selective inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces . FTI 277 HCl is effective in clearing HDV viremia.

Targets

FTase [1]
(Cell-free assay)
500 pM

In vitro

FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells. FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation.