Prexasertib (LY2606368) dihydrochloride | CHK1 Inhibitor

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CAS No. :	1234015-54-3
Formula :	C₁₈H₂₁Cl₂N₇O₂
M.W :	438.31
SMILES Code :	NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2.[H]Cl.[H]Cl
Synonyms :	LY2606368 dihydrochloride; LY2606368; Prexasertib HCl
MDL No. :	MFCD27918637
InChI Key :	KMEIPKXRCJTZBZ-UHFFFAOYSA-N
Pubchem ID :	46700755

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H335
Precautionary Statements:	P261-P305+P351+P338

human SCLC cell lines	300nM	72 hours	DDR targeting significantly increased the total level of PD-L1 protein in all cell lines tested with the greatest PD-L1 fold change (up to 5 fold) with prexasertib as detected by RPPA.	PMC6563834
H69, H446, RPP/mTmG cell lines	1μM	24 hours	Prexasertib treatment led to a significant (p<0.001) increase in MN frequency in treated samples.	PMC6563834
CRC-SCs	20 nM	72 hours	To evaluate the anti-CSC activity of Prexasertib on CRC-SCs, the results showed that Prexasertib exhibited significant anti-CSC activity in vitro on CRC-SCs.	PMC5890648
CRC-SCs	10 nM, 50 nM, 100 nM	1 hour, 4 hours, 9 hours, 24 hours	To evaluate the effect of Prexasertib on ATM phosphorylation levels in CRC-SCs, the results showed that Prexasertib significantly induced ATM phosphorylation in sensitive CRC-SCs.	PMC5890648
GLC4	30 nM	72 hours	To evaluate the cytotoxicity of Prexasertib in combination with cisplatin in SCLC cells, results showed that Prexasertib significantly enhanced the cytotoxicity of cisplatin.	PMC6534433
H792	30 nM	72 hours	To evaluate the cytotoxicity of Prexasertib in combination with cisplatin in SCLC cells, results showed that Prexasertib significantly enhanced the cytotoxicity of cisplatin.	PMC6534433
D283	15 nM	72 hours	LY2606368 showed synergistic effects with DNA-damaging agents (such as 4-HPC, CDDP, and GEM), significantly reducing the concentration of DNA-damaging drugs required to kill MB cells.	PMC8994821
D425	15 nM	72 hours	LY2606368 showed synergistic effects with DNA-damaging agents (such as 4-HPC, CDDP, and GEM), significantly reducing the concentration of DNA-damaging drugs required to kill MB cells.	PMC8994821
PEO1	0.5 nM	48 hours	Evaluate the inhibitory effect of Prexasertib on CHK1	PMC10758289
UWB	0.5 nM	48 hours	Evaluate the inhibitory effect of Prexasertib on CHK1	PMC10758289
CCRF-CEM cells	100 nM	4 hours	SLFN11 is recruited to chromatin and blocks replication in response to replication stress	PMC5802881
K562 cells	100 nM	2 hours	SLFN11, CDC45 and PCNA are enriched on nascent DNA under replication stress	PMC5802881
A549	100 nM	19 days	Screening for sgRNAs conferring resistance to Prexasertib	PMC7761918
H460	50 nM	19 days	Screening for sgRNAs conferring resistance to Prexasertib	PMC7761918
SCLC cell lines	300 nmol/L		To evaluate the antiproliferative effect of Prexasertib on SCLC cell lines, results showed that most SCLC cell lines were sensitive to Prexasertib	PMC5563854
NSCLC cell lines	>0.8 μmol/L		To evaluate the antiproliferative effect of Prexasertib on NSCLC cell lines, results showed that most NSCLC cell lines were resistant to Prexasertib	PMC5563854
AML cell lines (e.g., ML-1, THP.1, U937)	10 nM	24 hours	To evaluate the apoptotic effects of Prexasertib on AML cell lines, results showed that Prexasertib induced DNA fragmentation, phosphatidylserine exposure, and cleavage of caspase substrates, indicating apoptosis induction.	PMC8137540
U937 cells	10 nM	24 hours	To assess the role of CDC25A and CDK2 in CHK1 inhibitor-induced apoptosis, results showed that knockdown of CDC25A and CDK2 reduced CHK1 inhibitor-induced apoptosis.	PMC8137540
OVCAR8	5 nM	72 hours	To evaluate the effect of Prexasertib in combination with PI3K/mTOR inhibitor LY3023414 on cell viability, results showed that the combination treatment significantly reduced cell viability.	PMC7718416
PEO1	5 nM	72 hours	To evaluate the effect of Prexasertib in combination with PI3K/mTOR inhibitor LY3023414 on cell viability, results showed that the combination treatment significantly reduced cell viability.	PMC7718416
MCF-7	1 μM	24 hours	To evaluate the effect of Prexasertib on ERα expression levels, results showed that Prexasertib dose-dependently decreased ERα intracellular content.	PMC9006609
Y537S	1 μM	24 hours	To evaluate the effect of Prexasertib on ERα expression levels, results showed that Prexasertib dose-dependently decreased ERα intracellular content.	PMC9006609

mice	immunocompromised (nude) and immune competent (B6129F1) mouse models	subcutaneous injection	10 mg/kg	Twice weekly for 1 month	Prexasertib showed enhanced anti-tumor efficacy in the immunocompetent model (TC=0.13; p<0.0001) as compared to the immunocompromised model (T/C=0.47; p<0.01).	PMC6563834
mice	CRC-SCs xenograft model	subcutaneous injection	20 or 80 mg/kg	Single dose, sampling at 4, 8, and 24 hours post-dosing	To evaluate the anti-tumor effect of Prexasertib on CRC-SCs xenograft models, the results showed that Prexasertib significantly inhibited tumor growth in sensitive CRC-SCs.	PMC5890648
nude mice	SCLC xenograft model	subcutaneous injection	50 μg/kg caerulein and 15 mg/kg LPS	7 consecutive hourly injections (AEP) and 13 consecutive injections followed by one LPS injection (ANP)	To evaluate the antitumor activity of Prexasertib in combination with cisplatin in SCLC xenograft models, results showed that Prexasertib significantly enhanced the antitumor activity of cisplatin and overcame cisplatin resistance.	PMC6534433
mice	D425 G3-II MB orthotopic xenograft model	intravenous (i.v.) administration	10 mg/kg	Single dose 20 minutes before surgery	Combination of LY2606368 with CPM significantly extended the survival of mice and reduced tumor burden.	PMC8994821
Mice	NSG mice	Intraperitoneal injection	20 mg/kg	once per day for 6 weeks	Evaluate the therapeutic effect of Prexasertib on PARPi-resistant HGSC in vivo	PMC10758289
Mice	SCLC syngeneic model	Subcutaneous injection	10 mg/kg	every other day for 1 week	To evaluate the antitumor effect of Prexasertib as monotherapy and in combination with cisplatin in a SCLC syngeneic model, results showed significant tumor regression with Prexasertib monotherapy and enhanced effect with cisplatin combination	PMC5563854
Nude mice	AML xenograft model	Intraperitoneal injection	100 mg/kg	Three times a week for three weeks	To evaluate the antileukemic effects of Prexasertib in AML xenograft models, results showed that Prexasertib significantly inhibited tumor growth and prolonged host survival.	PMC8137540
NOD-SCID mice	OVCAR8 xenograft model	Intraperitoneal injection	105 PFU	Single injection, monitored for 10 days	To evaluate the effect of Prexasertib in combination with PI3K/mTOR inhibitor LY3023414 on tumor growth, results showed that the combination treatment significantly suppressed tumor growth.	PMC7718416

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CAS No.: 1234015-54-3

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CAS No.: 1234015-54-3

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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