Molibresib (I-BET762) | BRD4 Inhibitor

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CAS No. :	1260907-17-2
Formula :	C₂₂H₂₂ClN₅O₂
M.W :	423.90
SMILES Code :	O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
Synonyms :	I-BET-762; GSK525762; GSK525762A
MDL No. :	MFCD22417091
InChI Key :	AAAQFGUYHFJNHI-SFHVURJKSA-N
Pubchem ID :	46943432

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

BT474 cells	200 nM	3 days	To investigate the effect of Lapatinib on the expression of c-Myc and Bcl2, results showed that Lapatinib increased the mRNA levels of c-Myc and Bcl2	PMC4748715
MDA-MB-361 cells	50 nM	4 days	To investigate the effect of AKTi on the expression of c-Myc and Bcl2, results showed that AKTi increased the mRNA levels of c-Myc and Bcl2	PMC4748715
OCI-AML3	500 nM	6 hours	To evaluate the effect of I-BET151 on gene expression in NPM1c mutated AML cells, showing downregulation of BCL2 and C-MYC genes.	PMC3918873
SKM1	500 nM	6 hours	To evaluate the effect of I-BET151 on gene expression in EZH2 Y641C mutated AML cells, showing downregulation of BCL2 and C-MYC genes.	PMC3918873
H1373 cells	1 μM	24 hours	To evaluate the regulation of c-Myc expression by JQ1, finding that JQ1 significantly reduced c-Myc expression	PMC5059870
Eμ-myc B-cell lymphomas	0.5 μM	48 hours	Assessed I-BET762-induced cell death, results showed loss of plasma membrane integrity, loss of mitochondrial membrane potential, caspase activation, DNA fragmentation	PMC4720887
RAJI B-cell lymphomas	500-1000 nM	6-10 days	Assessed I-BET762-induced cell death, results showed loss of plasma membrane integrity, loss of mitochondrial membrane potential, caspase activation, DNA fragmentation	PMC4720887
RL B-cell lymphomas	500-1000 nM	6-10 days	Assessed I-BET762-induced cell death, results showed loss of plasma membrane integrity, loss of mitochondrial membrane potential, caspase activation, DNA fragmentation	PMC4720887
U2932 B-cell lymphomas	500-1000 nM	6-10 days	Assessed I-BET762-induced cell death, results showed loss of plasma membrane integrity, loss of mitochondrial membrane potential, caspase activation, DNA fragmentation	PMC4720887
SCLC cells	0.5 µM	24 hours	To evaluate the synergistic effect of BET inhibitors with PARP inhibitors, results showed synergy in SCLC cells with active MYC signaling pathway	PMC7766292
ALL-SIL	1 μM	6 hours	JQ1 and iBET both inhibited STAT5-dependent gene expression, while (−)-JQ1 had no effect	PMC4013223
DU528	1 μM	6 hours	JQ1 and iBET both inhibited the expression of STAT5 target genes	PMC4013223
HEL	0.5 μM	6 hours	JQ1 did not affect STAT5 phosphorylation	PMC4013223
BON cells	500 nM	5 days	IBET significantly inhibited the proliferation of BON cells and increased the protein level of p27, but did not affect its mRNA level.	PMC5450742
T98G	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
A549	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
HCT116	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
MDA-MB-231	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
DU145	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
MIAPaCa2	0.5, 2, 8, 32 nM CFZ	72 hours	BET inhibitors synergize with CFZ to induce cancer cell death	PMC7226130
FRO	5 μM	24 hours	To evaluate the effect of JQ1 on MCM5 mRNA expression, results showed significant downregulation of MCM5 mRNA.	PMC4891972
SW1736	5 μM	24 hours	To evaluate the effect of JQ1 on MCM5 mRNA expression, results showed significant downregulation of MCM5 mRNA.	PMC4891972
T4888M	0.5 μM	72 hours	To evaluate the effect of JQ1 on Mcm5 mRNA expression, results showed significant downregulation of Mcm5 mRNA.	PMC4891972
T3531L	0.5 μM	72 hours	To evaluate the effect of JQ1 on Mcm5 mRNA expression, results showed significant downregulation of Mcm5 mRNA.	PMC4891972

Nude mice	BT474 cell xenograft model	Oral and intraperitoneal injection	2.5 mg/kg	Every second day, three times	To investigate the effect of combined treatment with Lapatinib and IBET on HER2+ breast cancer xenografts, results showed that the combination significantly inhibited tumor growth	PMC4748715
mice	NPM1c AML model	intravenous injection	20 mg/kg	Once daily for 4 days	To evaluate the efficacy of I-BET151 in the NPM1c AML model, showing a significant survival advantage in treated mice.	PMC3918873
Mice	H1373 xenograft model	Intraperitoneal injection	Lapatinib 25 mg/kg, IBET 15 mg/kg	Lapatinib every other day, IBET daily, for 21 days	To evaluate the effects of JQ1 on tumor growth and c-Myc expression, finding that JQ1 significantly inhibited tumor growth and downregulated c-Myc expression	PMC5059870

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CAS No.: 1260907-17-2

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CAS No.: 1260907-17-2

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NCT03702036	-		-	-	-
NCT02706535	Drug Interactions	Phase 1	Completed	-	United States, Maryland ... More >> GSK Investigational Site Baltimore, Maryland, United States, 21225 Less <<
NCT03266159	Solid Tumours	Phase 2	Withdrawn(Study withdrawn befo... More >>re active to fully evaluate impact of changing practice in target population.) Less <<	August 19, 2020	-
NCT03150056	Solid Tumours	Phase 1	Recruiting	July 29, 2019	-
NCT02964507	Neoplasms	Phase 2	Recruiting	June 1, 2020	-
NCT01587703	Carcinoma, Midline	PHASE1	COMPLETED	2019-07-29	GSK Investigational Site, Balt... More >>imore, Maryland, 21231-2410, United States\|GSK Investigational Site, Boston, Massachusetts, 02215, United States\|GSK Investigational Site, Philadelphia, Pennsylvania, 19104, United States\|GSK Investigational Site, Nashville, Tennessee, 37232, United States\|GSK Investigational Site, Houston, Texas, 77030, United States\|GSK Investigational Site, Clayton, Victoria, 3168, Australia\|GSK Investigational Site, Bordeaux Cedex, 33076, France\|GSK Investigational Site, Lyon Cedex 08, 69373, France\|GSK Investigational Site, Paris Cedex 5, 75248, France\|GSK Investigational Site, Seoul, 03080, Korea, Republic of\|GSK Investigational Site, Seoul, 03722, Korea, Republic of\|GSK Investigational Site, Amsterdam, 1066 CX, Netherlands\|GSK Investigational Site, Barcelona, 08035, Spain\|GSK Investigational Site, Madrid, 28040, Spain\|GSK Investigational Site, Málaga, 29010, Spain\|GSK Investigational Site, Sutton, Surrey, SM2 5PT, United Kingdom\|GSK Investigational Site, Newcastle upon Tyne, NE7 7DN, United Kingdom Less <<
NCT01943851	Neoplasms	PHASE2	COMPLETED	2020-04-30	GSK Investigational Site, Litt... More >>le Rock, Arkansas, 72205, United States\|GSK Investigational Site, Aurora, Colorado, 80045, United States\|GSK Investigational Site, New York, New York, 10065, United States\|GSK Investigational Site, Philadelphia, Pennsylvania, 19104, United States\|GSK Investigational Site, Houston, Texas, 77030, United States\|GSK Investigational Site, East Melbourne, Victoria, 3002, Australia\|GSK Investigational Site, Seoul, 03722, Korea, Republic of\|GSK Investigational Site, Seoul, 06351, Korea, Republic of\|GSK Investigational Site, Barcelona, 08036, Spain\|GSK Investigational Site, Madrid, 28006, Spain\|GSK Investigational Site, Madrid, 28040, Spain\|GSK Investigational Site, Málaga, 29010, Spain\|GSK Investigational Site, Salamanca, 37007, Spain\|GSK Investigational Site, Cambridge, CB2 0QQ, United Kingdom\|GSK Investigational Site, London, W12 0NN, United Kingdom Less <<

Bio Calculators
Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.36mL 0.47mL 0.24mL	11.80mL 2.36mL 1.18mL	23.59mL 4.72mL 2.36mL
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

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