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CAS No. :	1462249-75-7
Formula :	C₁₈H₁₁F₃N₂O
M.W :	328.29
SMILES Code :	O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2
MDL No. :	MFCD28386154
InChI Key :	IAJOMYABKVAZCN-AATRIKPKSA-N
Pubchem ID :	71730058

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302
Precautionary Statements:	P280-P305+P351+P338

Acute myeloid leukemia cells	0.9 μM	96 hours	Evaluate the inhibitory effect of PFK158 combined with meclizine on AML cells, showing synergistic inhibition	J Hepatol. 2020 Apr;72(4):746-760.
HuH7 cells	2 or 5 μM	24 and 48 hrs	Evaluate the inhibitory effect of PFK158 combined with meclizine on the growth of liver cancer cells, showing synergistic inhibition	J Hepatol. 2020 Apr;72(4):746-760.
HepG2 cells	2 or 5 μM	24 and 48 hrs	Evaluate the inhibitory effect of PFK158 combined with meclizine on the growth of liver cancer cells, showing synergistic inhibition	J Hepatol. 2020 Apr;72(4):746-760.
DMS53 cells	0, 2.5, 5, 10 μM	24 hours	Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2	Oncogene. 2022 Aug;41(33):4003-4017.
H1876 cells	0, 2.5, 5, 10 μM	24 hours	Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2	Oncogene. 2022 Aug;41(33):4003-4017.
H1882 cells	0, 2.5, 5, 10 μM	24 hours	Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2	Oncogene. 2022 Aug;41(33):4003-4017.
H1048 cells	0, 2.5, 5, 10 μM	24 hours	Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2	Oncogene. 2022 Aug;41(33):4003-4017.
Patient-derived ascites cells	3-5µM	24 hours	To evaluate the effect of PFK158 on cell viability, results showed that PFK158 treatment reduced cell viability and restored primary cilia formation	J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
OVCAR5	10µM	24 hours	To evaluate the effect of PFK158 on primary cilia formation, results showed that PFK158 treatment significantly restored primary cilia formation	J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
OVCAR8	10µM	24 hours	To evaluate the effect of PFK158 on primary cilia formation, results showed that PFK158 treatment significantly restored primary cilia formation	J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
EMMeso	0-30μM	24 and 48 hours	PFK158 treatment inhibited MPM cell viability with IC50 values ranging from 3 to 12μM	Cell Death Dis. 2019 Sep 27;10(10):725.
NCI-H28	0-30μM	24 and 48 hours	PFK158 treatment inhibited MPM cell viability with IC50 values ranging from 3 to 12μM	Cell Death Dis. 2019 Sep 27;10(10):725.
OVCAR8 cells	5 µM	48 hours	To evaluate the effect of PFK158 on PARPi resistance, results showed that PFK158 inhibited PFKFB3 activity and enhanced PARPi sensitivity.	Cell Commun Signal. 2025 Jan 25;23(1):48.
SKOV3 cells	5 µM	48 hours	To evaluate the effect of PFK158 on PARPi resistance, results showed that PFK158 inhibited PFKFB3 activity and enhanced PARPi sensitivity.	Cell Commun Signal. 2025 Jan 25;23(1):48.
ARK-2	0-20 μM	24-72 hours	Inhibited cell proliferation, reduced glucose uptake, ATP production, and lactate dehydrogenase activity	Oncogene. 2021 Feb;40(8):1409-1424.
HEC-1B	0-20 μM	24-72 hours	Inhibited cell proliferation, reduced glucose uptake, ATP production, and lactate dehydrogenase activity	Oncogene. 2021 Feb;40(8):1409-1424.
HeyA8MDR	5μM	30 minutes	To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake	Int J Cancer. 2019 Jan 1;144(1):178-189.
HeyA8	5μM	30 minutes	To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake	Int J Cancer. 2019 Jan 1;144(1):178-189.
C13	5μM	30 minutes	To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake	Int J Cancer. 2019 Jan 1;144(1):178-189.
OV2008	5μM	30 minutes	To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake	Int J Cancer. 2019 Jan 1;144(1):178-189.
EMMeso	5 µM	24 hours	PFK158 treatment significantly increased p27 levels in EMMeso cells.	Br J Cancer. 2022 Oct;127(7):1352-1364.
NCI-H2052	2.5 µM	24 hours	PFK158 significantly decreased SOX2 and CD133 transcript levels in H2052 cells.	Br J Cancer. 2022 Oct;127(7):1352-1364.
NCI-H28	2.5 µM	24 hours	PFK158 significantly decreased SOX2, CD133 and CD44 transcript levels in H28 cells.	Br J Cancer. 2022 Oct;127(7):1352-1364.
DMS79	2.5 μM	72 hours	To evaluate the effect of PFK158 on ATP production, glucose uptake, and lactate secretion in MYC-low SCLC cell lines. Results showed that PFK158 had minimal effect on ATP production, glucose uptake, and lactate.	Cancer Metab. 2021 Sep 23;9(1):33.
H446	2.5 μM	72 hours	To evaluate the effect of PFK158 on ATP production, glucose uptake, and lactate secretion in MYC-high SCLC cell lines. Results showed that PFK158 significantly attenuated glucose uptake, ATP production, and lactate.	Cancer Metab. 2021 Sep 23;9(1):33.

SCID-NSG mice	H1048 CSC xenograft model	Intraperitoneally (ip)	25 mg/kg	Twice a week for 3 weeks	PFK158 treatment and PFKFB3 knockdown significantly reduced tumor growth and weight with reduced expression of cancer stem cell markers, ABCG2, and YAP/TAZ	Oncogene. 2022 Aug;41(33):4003-4017.
NOG mice	Human hepatocarcinoma cell line xenotransplantation model	Oral	25 mg/kg	Once daily for two weeks	Evaluate the inhibitory effect of PFK158 combined with meclizine on liver cancer growth, showing significant reduction in tumor burden	J Hepatol. 2020 Apr;72(4):746-760.
Female athymic nude mice	EMMeso xenograft model	Subcutaneous injection	30 mg/kg	Twice a week for 2 weeks	PFK158 alone or in combination with carboplatin significantly inhibited tumor growth	Cell Death Dis. 2019 Sep 27;10(10):725.
BALB/c nude mice	SKOV3 xenograft models	Intraperitoneally	35 mg/kg	Twice weekly for 28 days	To evaluate the in vivo efficacy of PFK158 combined with PARPi, results showed that the combination significantly inhibited tumor growth and increased DNA damage.	Cell Commun Signal. 2025 Jan 25;23(1):48.
Nude mice	HEC-1B and ARK-2 xenograft models	Intraperitoneal injection	35 mg/kg	Twice weekly for 14 days	Significantly inhibited tumor growth, reduced tumor volume and weight, and enhanced chemosensitivity	Oncogene. 2021 Feb;40(8):1409-1424.
Female athymic nude mice	Highly metastatic PTX-resistant ovarian mouse model	Intraperitoneal injection	25 mg/kg	PFK158 every 3rd day, CBPt every 3rd day, PTX every 5th day, for 28 days	To evaluate the effect of PFK158 alone or in combination with CBPt/PTX on tumor growth and ascites, results showed that the combination treatment significantly reduced tumor weight and ascites	Int J Cancer. 2019 Jan 1;144(1):178-189.
Female athymic nude mice	MPM xenograft model		30 mg/kg	Twice a week for 2 weeks	PFK158 significantly reduced tumour burden, tumour weight and tumour volume in TIC-mediated MPM xenografts.	Br J Cancer. 2022 Oct;127(7):1352-1364.
Mice	Apoe−/− mice	Intraperitoneal injection	2 mg/kg	3 times per week for 5 weeks	To evaluate the effect of PFK158 on plaque stability, results showed that PFK158 improved plaque stability.	Br J Pharmacol. 2022 Nov;179(21):4974-4991.
Nude mice	H446 xenograft model	Intraperitoneal injection	25 mg/kg	Every 2 days for a total of six treatments	To evaluate the effect of PFK158 on tumor growth in MYC-high SCLC xenograft models. Results showed that PFK158 significantly delayed tumor growth.	Cancer Metab. 2021 Sep 23;9(1):33.

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CAS No.: 1462249-75-7

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CAS No.: 1462249-75-7

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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