Dasatinib hydrochloride | Src/Bcr-Abl Inhibitor

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CAS No. :	854001-07-3
Formula :	C₂₂H₂₇Cl₂N₇O₂S
M.W :	524.47
SMILES Code :	O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C.[H]Cl
Synonyms :	BMS-354825 hydrochloride; Dasatinib hydrochloride; BMS-354825 HCl
MDL No. :	MFCD26960525
InChI Key :	MSCGWICDJYLQOJ-UHFFFAOYSA-N
Pubchem ID :	11466607

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

K562 chronic myeloid leukemia cells	0.1 nM	24 or 48 h	Dasatinib reduced the total exosome release from K562 cells	PMC3595015
SUM149	25 nM	24 and 72 h	Inhibit nEGFR translocation and enhance non-nuclear EGFR levels	PMC4013210
K562 leukemia cells	10nM		Inhibited BCR-ABL1 signaling and reduced leukemia stem cell self-renewal potential	PMC4975616
KG-1 cells	100 nM		Inhibit Src kinase activity and reduce cell proliferation	PMC3228896
BaF3 cells	10 nM and 100 nM	72 h	Inhibit Src kinase activity and reduce cell proliferation	PMC3228896
MDAMB468	25 nM	24 and 72 h	Inhibit nEGFR translocation and enhance non-nuclear EGFR levels	PMC4013210
SUM229	25 nM	24 and 72 h	Inhibit nEGFR translocation and enhance non-nuclear EGFR levels	PMC4013210
RL-95 cells	100 nM	48 h	Evaluate the effect of Dasatinib on p-p44/42 MAPK	PMC8511168
Normal CD34+ progenitors	10nM		Combined with JAK2 inhibitor to inhibit self-renewal potential	PMC4975616
SU-DHL-8 cells	100 nM	24 h	To assess the inhibitory effect of dasatinib on CD19-TCB-mediated target-cell killing. Results showed that 100 nM dasatinib significantly inhibited target-cell killing.	PMC8323395
MKN45 cells	100 nM	3 days	To assess the inhibitory effect of dasatinib on CEA-TCB-mediated target-cell killing. Results showed that 100 nM dasatinib significantly inhibited target-cell killing.	PMC8323395
A375 cells	100 nM	24 h	To assess the inhibitory effect of dasatinib on HLA-A2 WT1-TCB-mediated target-cell killing. Results showed that 100 nM dasatinib significantly inhibited target-cell killing.	PMC8323395
SKM-1 cells	50 nM	24 h	To assess the inhibitory effect of dasatinib on HLA-A2 WT1-TCB-mediated target-cell killing. Results showed that 50 nM dasatinib significantly inhibited target-cell killing.	PMC8323395
REH GCR cells	100-300 nM	48 h	Dasatinib combined with dexamethasone increased apoptosis, with Bliss synergy analysis showing additive effects (mean synergy score: 8.8).	PMC10203345
NALM6 cells	100-300 nM	48 h	Dasatinib combined with dexamethasone significantly increased apoptosis, with Bliss synergy analysis showing high synergy (mean synergy score: 30.8).	PMC10203345
PS125 cells	3nM or 10nM	24 h	Dasatinib alone at 3nM had no effect on PS125 cell viability, but showed synergistic effect when combined with AT9283.	PMC4179499
D556 cells	1, 5, 10, 50 and 100nM	1-24 h	Dasatinib markedly decreased p-Src levels, with near ablation of detectable p-Src following treatment with 5 and 10nM.	PMC4179499
DAOY cells	1, 5, 10, 50 and 100nM	1-24 h	Dasatinib markedly decreased p-Src levels, with near ablation of detectable p-Src following treatment with 5 and 10nM.	PMC4179499
human K562 cells	5 nM	48 h	Evaluate the effect of Dasatinib on cell viability, results showed Dasatinib fully suppressed cell growth	PMC4017764
human SUP-B15 cells	5 nM	48 h	Evaluate the effect of Dasatinib on cell viability, results showed Dasatinib fully suppressed cell growth	PMC4017764
mouse p190 BCR-ABL transformed hematopoietic progenitors	5 nM	48 h	Evaluate the effect of Dasatinib on cell viability, results showed Dasatinib fully suppressed cell growth	PMC4017764
human bone marrow-derived mesenchymal stem cells (BM-MSCs)	1 μM	21 days	To evaluate the effect of Dasatinib on adipogenesis in BM-MSCs. Results showed that Dasatinib reduced adipogenesis, decreasing the number and proportion of ORO-positive cells.	PMC10436421
Ishikawa cells	100 nM	48 h	Evaluate the effect of Dasatinib on p-p44/42 MAPK, results showed slight induction of pMAPK	PMC8511168
HEC-1A cells	100 nM	48 h	Evaluate the effect of Dasatinib on p-p44/42 MAPK, results showed slight induction of pMAPK	PMC8511168
Human umbilical vein endothelial cells (HUVEC)	10 nM	30 min	Dasatinib markedly inhibited HUVEC response to exosomes	PMC3595015

Humanized NSG mice	Humanized NSG mouse model	Oral	50 mg/kg	Three times on day 0 and twice on days 1 and 2	To assess the inhibitory effect of dasatinib on CD19-TCB-mediated B cell depletion and cytokine release. Results showed that 50 mg/kg dasatinib significantly inhibited B cell depletion and cytokine release.	PMC8323395
C7BL/6 mice	Mouse flank syngeneic MB tumor model	Oral gavage	15 mg/kg/day	Once daily for 5 consecutive days per week for 4 weeks	Dasatinib treatment resulted in significant reduction in MB tumor volume, with significantly lower tumor volumes compared to controls after 20 days of treatment.	PMC4179499
Mice	SUP-B15-luciferase xenograft model	Oral	2.5 mg/kg	Daily doses throughout the full treatment duration	Evaluate the effect of Dasatinib alone or in combination with PP242 on leukemic cell expansion, results showed combination treatment caused regression of leukemic disease	PMC4017764
Mice (BKS.Cg-+Leprdb/+Leprdb/OlaHsd (db/db))	Obese type 2 diabetes model	Oral gavage	5 mg/kg	Once per week for four weeks	To assess the effect of Dasatinib on cardiac lipid deposition and function. Results showed that Dasatinib reduced lipid accumulation in the heart and bone marrow, improved diastolic function indices (E/A ratio and non-flow time), and decreased cardiac fibrosis and expression of the senescence marker p16.	PMC10436421
Nude mice	HEC-1A orthotopic model	Oral	15 mg/kg	Daily until the end of the experiment	Evaluate the antitumor effect of Dasatinib alone or in combination with Trametinib, results showed that combination treatment significantly enhanced antitumor response	PMC8511168
RAG2−/−γc−/− mice	Humanized BC CML mouse model	Oral gavage	50 mg/kg	Daily for two weeks	Inhibited BC LSC survival and self-renewal, prolonged survival of serially transplanted mice	PMC4975616
BALB/c nude mice	Matrigel plug model	Oral	20 mg/kg	Once daily for 14 days	Dasatinib abrogated K562 exosome-induced angiogenesis	PMC3595015
Balb/c mice	ZNF112 and CEP2A cell transplantation model	Oral	20 mg/kg and 40 mg/kg	6 days per week for 4 weeks	Inhibit Src kinase activity and prolong survival	PMC3228896
Athymic nude mice	MDAMB468 xenograft model	Oral gavage	50 mg/kg	Once daily for 4 days	Inhibit nEGFR translocation and enhance membrane EGFR accumulation	PMC4013210

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CAS No.: 854001-07-3

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CAS No.: 854001-07-3

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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