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170006-73-2 (FTI-277)

1

Identification

FTI-277 FTI-277
Name FTI-277
Formula C22H29N3O3S2
MW 447.614
CAS No. 170006-73-2
EINECS
Smiles CSCC[[email protected]@H](C(OC)=O)NC(C1=CC=C(NC[[email protected]@H](N)CS)C=C1C2=CC=CC=C2)=O
Synonyms FTI-277,FTI277
InChI InChI=1S/C22H29N3O3S2/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26)/t16-,20+/m1/s1
2

Introduction

A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM; highly selective for FTase over GGTase I (IC50 = 50 nM); extremely potent (IC50=100 nM) at inhibiting H-Ras in whole cells; blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm.

Background Information

FTI 276 is an inhibitor that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines. ......by AdooQ BioScience, LLC
FTI-277, a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester deri ......by BOC Sciences
A peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM; highly selective for FTase over GGTase I (IC50 = 50 nM); extremely potent (IC50=100 nM) at inhibiting H-Ras in whole cells; blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm. ......by ProbeChem
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000012130

Storage condition

Solubility

5 mM in water by CHEMSCENE, LLC
5 mM in water by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Metabolic Enzyme/Protease
Target Farnesyl Transferase
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
FTI-277 - No Development Reported
7

Safety Data of FTI-277

Hazard Symbols : Xi
Risk Statements : 36/37/38
Safety Statements : 26-36
WGKGermany : 3
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Ark Pharm, Inc. USA
BOC Sciences
CHEMSCENE, LLC 5mg/USD288();10mg/USD540() USA
MedChemexpress Co., Ltd. 5mg/USD288();10mg/USD540() USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD288();10mg/USD540() China
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Related Products

Other Forms of 170006-73-2

Name CAS No Formula MW
FTI-277 (hydrochloride) 180977-34-8 C22H30ClN3O3S2 484.07

Recommended Compounds in Farnesyl Transferase

Name CAS No Formula MW
L-778123 183499-57-2 C22H20ClN5O 405.88
BMS-214662 195987-41-8 C25H23N5O2S2 489.61
Lonafarnib (Racemate) 193275-86-4 C27H31Br2ClN4O2 638.82
Lonafarnib (S enantiomer) 193275-85-3 C27H31Br2ClN4O2 638.82
Lonafarnib 193275-84-2 C27H31Br2ClN4O2 638.82
Tipifarnib 192185-72-1 C27H22Cl2N4O 489.4
L-778123 (hydrochloride) 253863-00-2 C22H21Cl2N5O 442.34
FTI-277 (hydrochloride) 180977-34-8 C22H30ClN3O3S2 484.07
Tipifarnib (S enantiomer) 192185-71-0 C27H22Cl2N4O 489.4
Chaetomellic acid A 148796-51-4 C19H34O4 326.47
Chaetomellic acid B 148796-52-5 C21H36O4 352.51
NPNPI-A C35H51N3O4S 609.86
NPNPI-B 276681-85-7 C33H51N3O4S 585.84
NPNPI-C C32H31N3O4S 553.67
CHEMBL505374 C41H49O13 749.82
CHEMBL1684849 C29H36ClFN2O5 547.06
CHEMBL258717 332131-42-7 C26H31N3O3 433.54
CHEMBL490300 1127735-76-5 C18H19O8PS 426.38
CHEMBL1685018 1292850-64-6 C30H36ClN2O7 572.07
CHEMBL142877 473987-17-6 C27H33ClN2O8 549.01

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

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More Information

FTI-277

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