UNC2025 | MER/FLT3 Inhibitor

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CAS No. :	1429881-91-3
Formula :	C₂₈H₄₀N₆O
M.W :	476.66
SMILES Code :	O[C@H]1CC[C@H](N2C=C(C3=CC=C(CN4CCN(C)CC4)C=C3)C5=CN=C(NCCCC)N=C52)CC1
MDL No. :	MFCD28142874
InChI Key :	MJSHVHLADKXCML-UHFFFAOYSA-N
Pubchem ID :	73425588

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

TRP	231.6 nM	5 days	Evaluate the inhibitory effect of UNC2025 on TRP cell growth, with an IC50 of 231.6 nM.	PMC5761530
EWS894 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
MHH-ES-1 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
Kasumi-1 AML cells	200-300nM	48 hours	Induced cell death, 25-90% of cells died after 48-hour treatment	PMC5354980
CHLA-32 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
GSC20	1.5 µM	5 days	Evaluate the inhibitory effect of UNC2025 on GSC20 cell growth, with an IC50 of 1.5 µM.	PMC5761530
GSC11	86 nM	5 days	Evaluate the inhibitory effect of UNC2025 on GSC11 cell growth, with an IC50 of 86 nM.	PMC5761530
SK-N-MC cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
CHLA-10 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
TC-71 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
A673 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
AML-123009 patient sample	25-300nM	48 hours	Inhibited colony formation, >90% inhibition at 300nM	PMC5354980
Jurkat T-ALL cells	200-300nM	48 hours	Induced cell death, 25-90% of cells died after 48-hour treatment	PMC5354980
697 B-ALL cells	200-300nM	48 hours	Induced cell death, 25-90% of cells died after 48-hour treatment	PMC5354980
M2 macrophages	1 µg/mL	2 hours	Inhibit MerTK phosphorylation and block efferocytosis of apoptotic cells	PMC10039929
EOC 2	199 nM	5 days	Evaluate the inhibitory effect of UNC2025 on EOC 2 cell growth, with an IC50 of 199 nM.	PMC5761530
J774	134 nM	5 days	Evaluate the inhibitory effect of UNC2025 on J774 cell growth, with an IC50 of 134 nM.	PMC5761530
TC-32 cells	1 μM	24 hours	UNC2025 suppressed SN-38-induced Akt and ERK signaling activation	PMC11192891
NOMO-1 AML cells	200-300nM	48 hours	Induced cell death, 25-90% of cells died after 48-hour treatment	PMC5354980
697 B-ALL cells	0.01, 0.1, 1.0, 10, 100, 1000 nM	10 minutes	Induced cell death, 25-90% of cells died after 48-hour treatment	PMC4148167
Bone marrow-derived dendritic cells (BMDCs)	10 µg/mL	12 hours	To evaluate the effect of Loratadine on dendritic cell antigen-presenting function, results showed that Loratadine significantly reduced the production of IL-4, IL-13, and IL-17A	PMC10039929
B16F10 melanoma cells	5 µM	6 hours	Cell apoptosis was assessed by FITC-Annexin V and TUNEL staining. Clofazimine induced apoptosis.	PMC10039929
Schwannoma cells	0.03-6.0 μM	72 hours and 7 days	UNC2025 decreased the total number of schwannoma cells, increased the number of dead cells, and reduced the proliferation of Ki67-positive cells.	PMC11458476
Meningioma cells	0.03-6.0 μM	72 hours and 7 days	UNC2025 decreased the total number of meningioma cells, increased the number of dead cells, and reduced the proliferation of Ki67-positive cells.	PMC11458476
Murine washed platelets	0.5 µM	15 minutes	Inhibited collagen-stimulated platelet aggregation	PMC5858881
Human platelet rich plasma (PRP)	5 µM	15 minutes	Inhibited collagen-stimulated platelet aggregation	PMC5858881
Human washed platelets (WP)	0.5 µM	15 minutes	Inhibited collagen-stimulated platelet aggregation	PMC5858881
Meningioma cells	1 µM	72 hours	UNC2025 decreased the total number of meningioma cells, increased the number of dead cells, and reduced the proliferation of Ki67-positive cells.	PMC10725030
MeWo	100 nM	72 hours	Reduction in survivin levels	PMC9787186
A101D	50 nM	10 days	Reduction in colony formation	PMC9787186
G361	1000 nM	90 minutes	Inhibition of MERTK activation and downstream signaling	PMC9787186
HMCB	300 nM	90 minutes	Inhibition of MERTK activation and downstream signaling	PMC9787186
H1299	300 nM	72 hours		PMC4704683
Colo699	300 nM	72 hours	To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis.	PMC4704683
A549	300 nM	72 hours	Evaluate cytotoxicity, showing low cytotoxicity	PMC4704683
H2228	300 nM	72 hours	To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis.	PMC4704683

Mice	TRP allograft model	Oral gavage	65 mg/kg	Once daily starting from day 7	Evaluate the effect of UNC2025 alone or in combination with radiotherapy on the survival of TRP allograft model mice. Results showed that UNC2025 alone did not significantly prolong survival, but when combined with radiotherapy, 19.4% of mice survived more than 60 days, with complete tumor regression in some mice.	PMC5761530
Nude mice	MHH-ES-1 xenograft model	Intraperitoneal injection	10 mg/kg	Every 3 days for 28 days	UNC2025 enhanced irinotecan's suppression of tumor growth	PMC11192891
NSG mice	697 B-ALL xenograft model	Oral	50-75mg/kg	Once daily, continuous treatment	Significantly reduced tumor burden, median survival increased from 26 days to 70 days	PMC5354980
NOD/SCID/gamma mice	Human leukemia xenograft model	Oral	3 mg/kg	Single dose, bone marrow cells collected 30 minutes later	To evaluate the inhibitory effect of UNC2025 on Mer phosphorylation in vivo, results showed significant reduction in Mer phospho-protein levels	PMC4148167
C57BL/6 mice	B16F10 melanoma model	Peritumoral injection	2.7 µg UNC2025/mouse	Every 3 days for two times	Inhibit tumor growth and metastasis, enhance antitumor immune responses	PMC10039929
Mice	FeCl3-Induced Carotid Artery Thrombosis model	Intravenous injection	3 mg/kg	Single dose, circulated for 30 minutes	Prolonged time to initial clot formation and decreased thrombus stability	PMC5858881
Male C57BL/6 mice	Hepatic ischemia-reperfusion injury model	Intravenous injection	50 mg/kg	Single dose, followed by reperfusion for up to 6 or 24 hours	UNC2025 significantly inhibited MSC-EVs-induced phagocytosis of apoptotic cells by macrophages and increased liver injury	PMC11387478
Nude mice	BRAF-mutated patient-derived xenograft model	Oral gavage	50 mg/kg	Twice daily for 50 days	Significantly reduced tumor growth	PMC9787186
Nude mice	Subcutaneous xenograft model	Oral gavage	30 mg/kg or 50 mg/kg	Twice daily for several weeks	To assess the effect of UNC2025 on tumor growth, results showed UNC2025 significantly inhibited tumor growth.	PMC4704683

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CAS No.: 1429881-91-3

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CAS No.: 1429881-91-3

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Biological Activity

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Precautionary Statements-General

Prevention

Response

Storage

Disposal

Physical hazards

Health hazards

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.10mL 0.42mL 0.21mL	10.49mL 2.10mL 1.05mL	20.98mL 4.20mL 2.10mL
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