FTI-277 hydrochloride | FTase Inhibitor

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CAS No. :	180977-34-8
Formula :	C₂₂H₃₀ClN₃O₃S₂
M.W :	484.07
SMILES Code :	CSCC[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl
Synonyms :	FTI-277 hydrochloride
MDL No. :	MFCD28385886
InChI Key :	PIAFFJUUNXEDEW-PXPMWPIZSA-N
Pubchem ID :	88309922

GHS Pictogram:
Signal Word:	Danger
Hazard Statements:	H302-H319-H332-H372-H400
Precautionary Statements:	P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:	9
UN#:	3077
Packing Group:	Ⅲ

Human mesenchymal stem cells (MSC)	5 μM and 10 μM	1 week and 3 weeks	FTI-277 significantly affected osteoblast differentiation (approx. -50±10%) and function (approx. -60±15%), with a higher inhibitory effect at 10 μM. Alendronate reversed the inhibitory effect of FTI-277.	PMC3051383
Human mesenchymal stem cells (MSC)	5 μM and 10 μM	2 weeks	Assessed the effect of FTI-277 on HDJ-2 and prelamin A, finding that FTI-277 inhibited farnesylation of both proteins, with a dose-dependent increase in unfarnesylated protein levels.	PMC3051383
HELN cells	10 µM	24 hours	In HELN cells, FTI-277 and GGTI-298 stimulated basal transcriptional activity by 3.6-fold and 2.4-fold, respectively, in the absence of E2. In the presence of E2, FTI-277 and GGTI-298 further enhanced transcriptional activity by an additional 2.2-fold and 1.6-fold, respectively.	PMC1064103
MCF-7 cells	10 µM	24 hours	FTI-277 significantly enhanced E2-induced transcriptional activity. In the absence of E2, FTI-277 and GGTI-298 stimulated basal transcriptional activity by 8.4-fold and 3.9-fold, respectively. In the presence of E2, FTI-277 and GGTI-298 further enhanced transcriptional activity by an additional 4.1-fold and 2.5-fold, respectively.	PMC1064103
ESC-derived VEGFR2+ cells	3 μM	4 days	Under low-density culture conditions, FTI-277 significantly reduced PECAM1+ colony numbers and increased αSMA+ colonies, indicating specific inhibition of endothelial differentiation.	PMC2287293
MCF7 breast cancer cells	5 μM	48 hours	Combined use of FTI-277 and IPA3 did not significantly inhibit cell proliferation	PMC3765434
A549 lung cancer cells	5 μM	48 hours	Combined use of FTI-277 and IPA3 significantly inhibited cell proliferation	PMC3765434
HT29 colon cancer cells	5 μM	48 hours	Combined use of FTI-277 and IPA3 significantly inhibited cell proliferation	PMC3765434
A375MM melanoma cells	5 μM or 15 μM	48 hours	FTI-277 treatment did not affect PAK protein levels but increased nuclear PhoPAK clusters	PMC3765434
HeLa cells	5 μM or 15 μM	48 hours	After 48 h of FTI-277 treatment, PAK and PhoPAK signals significantly increased	PMC3765434
SH-SY5Y cells	100 nM	48 hours	Reduced the abundance of membrane-associated UCH-L1 (UCH-L1M), decreased α-synuclein levels, and increased cell viability	PMC2651203
MCF-7 cells	10 μM	48 hours	To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of MCF-7 cells.	PMC7291698
4T1 cells	10 μM	48 hours	To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of 4T1 cells.	PMC7291698
67NR cells	10 μM	48 hours	To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of 67NR cells.	PMC7291698
ESC-derived VEGFR2+ cells	1 μM	48 hours	FTI-277 added within 3 hours post-VEGF-A stimulation suppressed endothelial differentiation, but no effect when added after 6 hours, demonstrating time-dependent inhibition.	PMC2287293
B16F10 melanoma cells	10 or 20 μM	48 hours	FTI-277 did not enhance membrane FasL expression	PMC2134904
Human bronchial mesenchymal fibroblasts	10 μM	48 hours	To investigate the effect of FTI-277 on TGFβ1-induced fibronectin expression; results showed no significant inhibition of fibronectin accumulation	PMC3173339
MCF-7 cells	5.9 nM	5 days	To evaluate the inhibitory effects of FTI-277 in combination with different anti-estrogens on MCF-7 cell proliferation. Results showed that FTI-277 combined with Tam had an additive effect, while combinations with ICI182,780 or PBPE exhibited synergistic effects.	PMC1410750
CNE1 cells	1 μM	72 hours	FTI-277 in combination with cisplatin slightly enhanced cytotoxicity in NPC cells with medium CENP-F expression	PMC2944187
HONE1 cells	1 μM	72 hours	FTI-277 in combination with cisplatin significantly enhanced cytotoxicity in NPC cells with high CENP-F expression	PMC2944187
Murine bone marrow-derived mast cells	5 μM	72 hours	Inhibition of Ras isoprenylation significantly reduces mast cell degranulation, cytokine production, and migration	PMC7655736
3T3-L1 cells	20 µM(first 24 h), then 2.5 µM (next 7 days)	8 days	To investigate the effect of FTI-277 on adipogenesis in 3T3-L1 cells. Results showed that FTI-277 increased the number of mature adipocytes, but when combined with non-farnesylated prelamin A accumulation, it reduced the expression of adipogenic genes.	PMC10816192
CHO-K1 cells	1 μM	8 hours	An 8 h treatment with 1μM FTI-277 led to an increase in p27 expression in cells that were selected before analysis for H-2Kk expression on magnetic beads conjugated to a monoclonal antibody against H-2Kk.	PMC1299091
HeLa cells	1 μM	8 hours	Addition of FTI-277 resulted in a 10- to 20-fold increase in LucF translation with a reporter containing the R17-binding site.	PMC1299091
SK-Hep1 cells	1 μM	8 hours	FTI-277 prevents the membrane association of the CAAX motif and thus increases the cytoplasmic levels of the eIF4G fusion protein, which is then capable of inducing translation of the second cistron of a bicistronic messenger RNA containing an R17-binding site in its intercistronic space.	PMC1299091
COS-7 cells	100 nM		Decreased the amount of transfected WT UCH-L1M	PMC2651203

Mouse	E6.75 whole-embryo culture model	In vitro culture medium	10 μM	Single dose, cultured for 3 days	FTI-277 treatment diminished PECAM1+ vessels in yolk sacs, with decreased PECAM1 and VE-cadherin mRNA levels but unchanged αSMA expression, suggesting suppression of vascular development.	PMC2287293
Mouse	Dopaminergic neurons in midbrain mixed primary cultures	Added to culture medium	100 nM	Single treatment, duration not specified	Reduced α-synuclein toxicity	PMC2651203
Mice	HBV transgenic mice	Intraperitoneal injection	50 mg/kg/day	Once daily for 7 days	FTI-277 and FTI-2153 were both highly effective at clearing HDV viremia	PMC166292

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CAS No.: 180977-34-8

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CAS No.: 180977-34-8

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.07mL 0.41mL 0.21mL	10.33mL 2.07mL 1.03mL	20.66mL 4.13mL 2.07mL
Dissolving Methods	Animal experiment Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn: in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1 Protocol 2 The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed