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CAS No. :	5291-32-7
Formula :	C₁₀H₁₇NO₃
M.W :	199.25
SMILES Code :	O=C1C(COC)(CO)N2CCC1CC2
Synonyms :	PRIMA-1Met; APR-246; APR 246. PRIMA-1MET
MDL No. :	MFCD16294187
InChI Key :	BGBNULCRKBVAKL-UHFFFAOYSA-N
Pubchem ID :	52918385

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H335
Precautionary Statements:	P261-P280-P301+P312-P302+P352-P305+P351+P338

BT-20	100 µM	12 hours	APR-246 enhanced the expression of IFN signalling genes	Br J Cancer. 2022 Nov;127(11):2060-2071.
BT-549	40 µM	12 hours	APR-246 enhanced the expression of IFN signalling genes	Br J Cancer. 2022 Nov;127(11):2060-2071.
DLD-1	90 µM	24 hours	APR-246 enhanced the expression of IFN signalling genes	Br J Cancer. 2022 Nov;127(11):2060-2071.
Recombinant rat TrxR1	50 µM	10 minutes	APR-246 inhibits TrxR1 activity, with MQ and preheated APR-246 being more potent inhibitors.	Cell Death Dis. 2013 Oct 24;4(10):e881.
SKBR-3	40 µM	12 hours	APR-246 repressed the expression of immune checkpoint molecules	Br J Cancer. 2022 Nov;127(11):2060-2071.
MDAMB-231	200 µM	12 hours	APR-246 repressed the expression of immune checkpoint molecules	Br J Cancer. 2022 Nov;127(11):2060-2071.
MDAMB-468	60 µM	12 hours	APR-246 repressed the expression of immune checkpoint molecules	Br J Cancer. 2022 Nov;127(11):2060-2071.
OACM5.1 cells	50 µM	12 hours	To study the effect of Eprenetapopt on cellular metabolism, results showed that Eprenetapopt decreased reduced GSH levels without increasing oxidized GSH (GSSG) levels, indicating total GSH depletion.	Sci Adv. 2022 Sep 16;8(37):eabm9427.
MOLM14	60 µM	16 hours	To investigate the mechanisms underlying APR-246-induced cell death, results showed that iron chelators and lipophilic antioxidants almost completely rescued cell viability, indicating that cell death is both iron and ROS-dependent.	Haematologica. 2022 Feb 1;107(2):403-416.
OVCAR-3	0.0025, 0.01, 0.05, 0.2, 0.8, 3.1, 12.5 µM	2 hours	MS-CETSA data indicated that ASNS is a direct or indirect target of APR-246 via the active product MQ. MQ treatment resulted in increased thermal stability of ASNS, suggesting that MQ may directly or indirectly affect ASNS activity.	Cell Death Dis. 2021 Jul 15;12(7):709.
CCRF-CEM	10, 15 µM	2 hours	WB-CETSA results showed that MQ treatment induced a temperature-dependent stabilization of ASNS at 57 and 59 °C, indicating that MQ directly or indirectly modulates ASNS.	Cell Death Dis. 2021 Jul 15;12(7):709.
Neuroblastoma cell lines	16.1 µM	24 hours	To investigate the ability of PRIMA-1MET to induce NB cell death, results showed that PRIMA-1MET induces cell death at low concentrations	J Exp Clin Cancer Res. 2019 Feb 12;38(1):69.
Keratinocytes	65.8 µM (IC50)	24 hours	To compare the specificity of PRIMA-1MET for tumor cells versus normal cells, results showed that normal cells are less sensitive to PRIMA-1MET	J Exp Clin Cancer Res. 2019 Feb 12;38(1):69.
Fibroblasts	78.3 µM (IC50)	24 hours	To compare the specificity of PRIMA-1MET for tumor cells versus normal cells, results showed that normal cells are less sensitive to PRIMA-1MET	J Exp Clin Cancer Res. 2019 Feb 12;38(1):69.
H1299 cells	50 µM	24 hours	To investigate whether Eprenetapopt-induced cell death could be reversed by ferroptosis inhibitors, results showed that ferroptosis inhibitors could reverse Eprenetapopt-induced cell death.	Sci Adv. 2022 Sep 16;8(37):eabm9427.
HL60	11 µM to >200 µM	24 hours	To evaluate the activity of APR-246 in AML cells, results showed that most AML cell lines and primary AML cells were sensitive to cell death induction by APR-246.	Haematologica. 2022 Feb 1;107(2):403-416.
TE1	10.5 µM	48 hours	APR-246 induced significant apoptosis by upregulating p73 and Noxa via ROS induction in ESCC cell lines harbouring p53 missense mutations.	Br J Cancer. 2021 Nov;125(11):1523-1532.
KYSE410	31.6 µM	48 hours	APR-246 showed minimal effectiveness in ESCC with wild-type p53, and did not significantly induce apoptosis.	Br J Cancer. 2021 Nov;125(11):1523-1532.
FLO-1	25 µM(GI90)	6 hours	To detect intracellular ROS levels after APR-246 treatment, results showed that APR-246 significantly increased ROS levels in FLO-1 cells.	Nat Commun. 2017 Mar 28;8:14844.
JH-EsoAd1	40 µM(GI90)	6 hours	To detect intracellular ROS levels after APR-246 treatment, results showed that APR-246 significantly increased ROS levels in JH-EsoAd1 cells.	Nat Commun. 2017 Mar 28;8:14844.
Keratinocytes from EEC syndrome patients	10–30 µM	7 days	APR-246 partially restored differentiation defects in p63 mutant keratinocytes	Proc Natl Acad Sci U S A. 2013 Feb 5;110(6):2157-62.
UMSCC10A	0-50 µM	72 hours	To evaluate the effect of APR-246 combined with PL on HNSCC cells, the results showed that the combination significantly reduced cell viability and increased cell death.	Oncogene. 2018 Jun;37(25):3384-3398.
FaDu	0-50 µM	72 hours	To evaluate the effect of APR-246 combined with PL on HNSCC cells, the results showed that the combination significantly reduced cell viability and increased cell death.	Oncogene. 2018 Jun;37(25):3384-3398.
A2780-CP20	8 µM, 20 µM, 30 µM, 40 µM, 60 µM	72 hours	APR-246 completely restored the sensitivity of ovarian cancer cells to cisplatin at clinically relevant concentrations.	Cell Death Dis. 2015 Jun 18;6(6):e1794.
OVCAR-3	2 µM, 20 µM, 30 µM	72 hours	APR-246 resensitized OVCAR-3 cells to cisplatin and increased the efficacy of cisplatin.	Cell Death Dis. 2015 Jun 18;6(6):e1794.
Neuroblastoma cells	3.8 µM	96 hours	To assess the cytotoxicity of APR-246 on ALT cells, results showed ALT cells were significantly more sensitive to APR-246	Cancer Res. 2022 Sep 16;82(18):3345-3358.
Rhabdomyosarcoma cells	3.8 µM	96 hours	To assess the cytotoxicity of APR-246 on ALT cells, results showed ALT cells were significantly more sensitive to APR-246	Cancer Res. 2022 Sep 16;82(18):3345-3358.
Carcinoma cells	3.8 µM	96 hours	To assess the cytotoxicity of APR-246 on ALT cells, results showed ALT cells were significantly more sensitive to APR-246	Cancer Res. 2022 Sep 16;82(18):3345-3358.
FLO-1 cells	50 μM	24 hours	Evaluate eprenetapopt-induced cell death, results showed ferroptosis inhibitors could reverse cell death	Sci Adv. 2022 Sep 16;8(37):eabm9427.
H1299 cells	50 μM	24 hours	Evaluate eprenetapopt-induced cell death, results showed ferroptosis inhibitors could reverse cell death	Sci Adv. 2022 Sep 16;8(37):eabm9427.
OACM5.1 cells	50 μM	12 hours	Evaluate the effect of eprenetapopt on GSH levels, results showed decreased GSH levels	Sci Adv. 2022 Sep 16;8(37):eabm9427.
OVCAR-3 ovarian cancer cells	2-30 μM	72 hours	APR-246 increased the sensitivity of OVCAR-3 cells to cisplatin and reduced the survival index plateau at higher concentrations.	Cell Death Dis. 2015 Jun 18;6(6):e1794.
A2780-CP20 ovarian cancer cells	8-60 μM	72 hours	APR-246 completely restored the sensitivity of ovarian cancer cells to cisplatin at clinically relevant concentrations.	Cell Death Dis. 2015 Jun 18;6(6):e1794.

Mice	FLO-1 xenograft model	Intraperitoneal injection	100 mg/kg	Once daily for 3 weeks	To evaluate the anti-tumour activity of APR-246 in the FLO-1 xenograft model, results showed that APR-246 significantly inhibited tumour growth.	Nat Commun. 2017 Mar 28;8:14844.
BALB/C mice	MCO4 fibrosarcoma model	Intraperitoneal injection	100 mg/kg	Daily for 4 days	APR-246 promoted CD4+ T cells infiltration and decreased the exhaustion of CD8+ T cells in vivo	Br J Cancer. 2022 Nov;127(11):2060-2071.
NSG mice	FLO-1 LM tumor model	Intraperitoneal injection	100 mg/kg	Daily for 35 days	To study the effect of Eprenetapopt combined with serine and glycine dietary restriction on tumor growth, results showed that the combination significantly inhibited primary tumor growth and delayed the onset of metastatic disease.	Sci Adv. 2022 Sep 16;8(37):eabm9427.
NOD/SCID IL-2 receptor γ-chain-null mice	MOLM14 xenograft model	Intraperitoneal injection	100 mg/kg	Once daily for 4 days	To evaluate the synergistic anti-leukemic activity of APR-246 combined with SLC7A11 inhibition, results showed that SLC7A11 knockdown significantly reduced tumor cell burden in the BM, and this effect was enhanced when combined with APR-246 treatment.	Haematologica. 2022 Feb 1;107(2):403-416.
C57BL/6J mice	B16 melanoma model	Intraperitoneal injection	100 mg/kg	Daily for 6 days	To study the effects of APR-246 on p53 expression in the tumor microenvironment and its combination with immune checkpoint blockade	J Clin Invest. 2022 Sep 15;132(18):e148141
SCID mice	UMSCC10A xenograft model	Intraperitoneal injection	100 mg/kg/day	Daily for 24 days	To evaluate the effect of APR-246 combined with PL on HNSCC xenograft tumors, the results showed that the combination significantly suppressed tumor growth.	Oncogene. 2018 Jun;37(25):3384-3398.
Mice	Xenograft model	Intraperitoneal injection	25 mg/kg/day	Once daily for 21 days	Combination of APR-246 and 5-FU showed synergistic antitumour effects in p53 missense mutant ESCC xenograft models through activation of ROS and the p73-Noxa pathway.	Br J Cancer. 2021 Nov;125(11):1523-1532.
Athymic nu/nu mice	Xenograft model	Intraperitoneal injection	250 mg/kg	Twice daily for 7 days, 21-day cycle, total of 3 cycles	To evaluate the efficacy of APR-246 combined with irinotecan in ALT xenograft models, results showed complete responses in ALT models	Cancer Res. 2022 Sep 16;82(18):3345-3358.
Mice	A2780-CP20 tumor xenograft model	Intravenous injection	400 mg/kg/day	APR-246: once daily for 7 days; cisplatin: once on day 2 and day 6	APR-246 in combination with cisplatin significantly inhibited tumor growth, indicating at least an additive effect.	Cell Death Dis. 2015 Jun 18;6(6):e1794.
Mice	Eso26 esophageal cancer cell xenograft model	Intraperitoneal injection	50 mg/kg APR-246, 50 mg/kg MK-571	APR-246 daily for 16 days; MK-571 daily except on days 6–7 and 13–14	Combination treatment with APR-246 and MK-571 significantly suppressed the growth of Eso26 xenograft tumors and prolonged the survival of mice.	EMBO Mol Med. 2021 Feb 5;13(2):e10852
NSG mice	FLO-1 LM xenograft model	Intraperitoneal injection	100 mg/kg	Daily for 35 days	Evaluate the effect of combining eprenetapopt with serine and glycine dietary restriction, results showed combination therapy significantly inhibited tumor growth	Sci Adv. 2022 Sep 16;8(37):eabm9427.

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CAS No.: 5291-32-7

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CAS No.: 5291-32-7

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NCT00900614	Hematologic Neoplasms\|Prostati... More >>c Neoplasms Less <<	PHASE1	COMPLETED	2025-10-10	Section of Haematology and Coa... More >>gulation, Sahlgrenska University Hospital, G?teborg, 41345, Sweden\|Hematology Centre, M54, Karolinska Institute, Karolinska University Hospital, Huddinge, Stockholm, SE 141 86, Sweden\|Clinical Research and Development Unit, Department of Oncology, Akademiska Hospital, Uppsala, 75185, Sweden\|Department of Haematology, Akademiska Hospital, Uppsala, 75185, Sweden\|Department of Hematology, University Hospital, ?rebro, 70185, Sweden\|Urology clinic, University Hospital, ?rebro, 70185, Sweden Less <<
NCT03931291	Acute Myeloid Leukemia or Myel... More >>odysplastic Syndromes Less <<	PHASE2	COMPLETED	2022-01-14	H. Lee Moffitt Cancer Center &... More >> Research Institute, Tampa, Florida, 33612, United States\|Johns Hopkins, Sidney Kimmel Comprehensive Cancer Center, Baltimore, Maryland, 21278, United States\|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States\|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States\|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States\|Vanderbilt Ingram Cancer Center, Nashville, Tennessee, 37232, United States\|Fred Hutchinson Cancer Center, Seattle, Washington, 98109, United States Less <<
NCT02999893	Oesophageal Carcinoma	PHASE1\|PHASE2	TERMINATED	2021-02-07	Monash Medical Centre, Clayton... More >>, Victoria, 3000, Australia\|Austin Health, Heidelberg, Victoria, 3000, Australia\|Peter MacCallum Cancer Centre, Melbourne, Victoria, 3002, Australia\|Alfred Hospital, Prahran, Victoria, 3000, Australia\|Sunshine Hospital Western Health, Sunshine, Victoria, 3000, Australia Less <<

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