FRAX1036 | PAK Inhibitor

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CAS No. :	1432908-05-8
Formula :	C₂₈H₃₂ClN₇O
M.W :	518.05
SMILES Code :	O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC
MDL No. :	MFCD30187513
InChI Key :	RYCBSFIKWACFBY-UHFFFAOYSA-N
Pubchem ID :	71557891

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

8505C	>10 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
Madin-Darby canine kidney cells (MDCK)	10 μM	60 minutes	Evaluated permeability with Papp value of 1.2×10−6 cm/s	PMC4677365
SW1736	>10 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
HTh74	6.14 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
BCPAP	7.73 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
TPC1	3.94 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
U2OS	2.5 μM FRAX1036, 0.2 μM docetaxel	20 hours	To evaluate the effect of FRAX1036 and docetaxel on microtubule organization and cell fate, disorganized microtubules and increased apoptosis were observed.	PMC4445529
HCC2911	5 μM FRAX1036, 0.2 μM docetaxel	24 hours	To evaluate the effect of FRAX1036 and docetaxel combination on apoptosis, increased apoptotic markers (cleaved PARP) and decreased cell cycle regulators (cyclin D1) were observed.	PMC4445529
THJ-16T	>10 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
FTC133	>10 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
K1	>10 μM	72 hours	Reduced thyroid cancer cell viability	PMC7062234
MDA-MB-175	0.5, 1, 2.5, 5 μM	24 hours	To evaluate the effect of FRAX1036 on PAK1 effector signaling and cell survival, inhibition of PAK1 effector signaling (MEK1-S298 and CRAF-S338) was observed to correlate with PARP cleavage.	PMC4445529
SW480	3 μM	25 days	To evaluate the effect of FRAX1036 on SW480 cell proliferation, results showed that SW480 cells regrew after 25 days of prolonged exposure to FRAX1036.	PMC10539494
HCT116	1 μM	21 days	To evaluate the effect of FRAX1036 on HCT116 cell proliferation, results showed that HCT116 cells regrew after 21 days of prolonged exposure to FRAX1036.	PMC10539494
T47D	IC50 5.0–11.5 µM	72 hours	Evaluate the anti-proliferative effect of FRAX1036 in T47D cells, showing lower activity in luminal cell lines.	PMC6661032
BT474	IC50 5.0–11.5 µM	72 hours	Evaluate the anti-proliferative effect of FRAX1036 in BT474 cells, showing lower activity in luminal cell lines.	PMC6661032
MCF7	IC50 5.0–11.5 µM	72 hours	Evaluate the anti-proliferative effect of FRAX1036 in MCF7 cells, showing lower activity in luminal cell lines.	PMC6661032
A549 cells	10 μM	24-48 hours	To evaluate the effect of FRAX1036 on the morphology, motility, and proliferation of A549 cells. Results showed that FRAX1036 combined with prenylation inhibitors significantly altered cell morphology and motility, and reduced cell proliferation.	PMC4477307
H157 cells	10 μM	24-48 hours	To evaluate the effect of FRAX1036 on the morphology, motility, and proliferation of H157 cells. Results showed that FRAX1036 combined with prenylation inhibitors significantly altered cell morphology and motility, and reduced cell proliferation.	PMC4477307
MS02 cells	0.6 μM, 1.2 μM, 2.5 μM, 5.0 μM	2 hours	To evaluate the inhibitory effect of FRAX-1036 on PAK1 phosphorylation, results showed a profound inhibitory effect on PAK1 autophosphorylation.	PMC8369838

Nude mice	MPNST subcutaneous xenograft model	Oral	30 mg/kg/day	Once daily for 4 weeks	To evaluate the inhibitory effect of Frax1036 alone or in combination with MEK1/2 inhibitor PD-901 on MPNST xenograft growth, results showed the combination therapy significantly inhibited tumor growth	PMC5608634
NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice	BT474 orthotopic xenografts	Oral gavage	20 mg/kg daily	Daily for 21 days	Evaluate the anti-tumor effect of FRAX1036 in BT474 xenograft model, showing significant tumor growth inhibition when combined with alisertib.	PMC6661032
Mice	H292 NSCLC xenograft model	Oral	10, 20, 30 mg/kg	Single dose, samples collected 6 hours post-dose	Assessed inhibition of pharmacodynamic biomarker pMEK S298, showing dose-dependent suppression	PMC4677365
Mice	Nf2 conditional knockout mouse model	Oral gavage	30 mg/kg	Once daily for 12 weeks	To evaluate the efficacy of FRAX-1036 in slowing the growth of established schwannomas, results showed insignificant efficacy in vivo.	PMC8369838

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CAS No.: 1432908-05-8

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CAS No.: 1432908-05-8

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Precautionary Statements-General

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Response

Storage

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	1.93mL 0.39mL 0.19mL	9.65mL 1.93mL 0.97mL	19.30mL 3.86mL 1.93mL
Dissolving Methods	Animal experiment 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