Almonertinib (HS-10296) | EGFR-sensitizing/T790M Inhibitor

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CAS No. :	1899921-05-1
Formula :	C₃₀H₃₅N₇O₂
M.W :	525.64
SMILES Code :	C=CC(NC1=CC(NC2=NC=CC(C3=CN(C4CC4)C5=C3C=CC=C5)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
Synonyms :	HS-10296; Ameile; Aumolertinib
MDL No. :	MFCD32173681

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

LU0387 cells	312 nM	7 days	Evaluate the inhibitory effect of Almonertinib on the proliferation of LU0387 cells with EGFR NPH mutation	PMC10326255
Human NSCLC cell lines HCC827	0.0003, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM	72 h	To determine the IC50 of Almonertinib on HCC827 cells, results showed significant inhibitory effects in EGFR-del19 mutant cells.	PMC9063085
Human NSCLC cell lines H1975	0.01, 0.1, 1, 10, 20, 50, 100 μM	72 h	To determine the IC50 of Almonertinib on H1975 cells, results showed significant inhibitory effects in EGFR L858R/T790M mutant cells.	PMC9063085
Human NSCLC cell lines A549	1, 2, 5, 10, 20, 50, 100 μM	72 h	To determine the IC50 of Almonertinib on A549 cells, results showed weak inhibitory effects in EGFR wild-type cells.	PMC9063085
HCC827/AR cells	8 μM	24 h	To evaluate the effects of Almonertinib combined with Baicalein on cell proliferation and apoptosis. Results showed that the combination significantly inhibited cell proliferation and induced apoptosis.	PMC11322074
H1975/AR cells	8 μM	24 h	To evaluate the effects of Almonertinib combined with Baicalein on cell proliferation and apoptosis. Results showed that the combination significantly inhibited cell proliferation and induced apoptosis.	PMC11322074
BCRP-MDCK monolayer cells	1, 10, 20 μM	4 h	To study the transport characteristics of Almonertinib in BCRP-MDCK cells, results showed an efflux ratio of 4.62 at 1 μM concentration	PMC8497791
ABCB1-MDCK monolayer cells	1, 10, 20 μM	4 h	To study the transport characteristics of Almonertinib in ABCB1-MDCK cells, results showed an efflux ratio of 5.2 at 1 μM concentration	PMC8497791

BALB/c nude mice	Ba/F3 EGFR ASV and L861Q allografts model	Oral	20 and 40 mg/kg	Once daily for 13 days	Evaluate the inhibitory effect of Almonertinib on tumor growth with EGFR ASV and L861Q mutations	PMC10326255
Balb/c nude mice	H1975 and HCC827 xenograft model	Oral	20 mg/kg	Once daily, multiple cycles (4 days per cycle)	To evaluate the anti-tumor effect of Almonertinib in H1975 and HCC827 xenograft models, results showed that P-A sequence (pemetrexed followed by Almonertinib) exhibited significant synergistic anti-tumor effects.	PMC9063085
BALB/c nude mice	Subcutaneous HCC827/AR cell xenograft model		15 mg/kg	24 days	To evaluate the inhibitory effects of Almonertinib combined with Baicalein on tumor growth. Results showed that the combination significantly inhibited tumor growth.	PMC11322074
BALB/c nude mice	PC9-LUC brain and spinal cord metastasis models	Oral	5, 10, 25 mg/kg	Once daily for 60 days	To evaluate the anti-tumor efficacy of Almonertinib in brain and spinal cord metastasis models, results showed that 25 mg/kg Almonertinib significantly inhibited tumor growth and prolonged survival time	PMC8497791
Rats	Healthy SD rats	Oral	15 mg/kg	For nine consecutive days	To evaluate the pharmacokinetic interactions between almonertinib and rivaroxaban or apixaban. Results showed that almonertinib significantly increased the plasma concentration and AUC of rivaroxaban and apixaban, and decreased their clearance.	PMC10582335

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CAS No.: 1899921-05-1

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CAS No.: 1899921-05-1

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Precautionary Statements-General

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NCT04785742	Safety of Almonertinib	PHASE2	UNKNOWN	2023-12-31	Sun Yat-sen University Cancer ... More >>Center, Guangzhou, Guang Dong, China Less <<
NCT04952168	NSCLC, Stage III	PHASE2	UNKNOWN	2023-06-02	Tongji Hospital of Tongji Medi... More >>cal College of Huazhong University of Science and Technology, Wuhan, Hubei, 430030, China Less <<
NCT04922138	Lung Cancer	PHASE2	RECRUITING	2025-10-15	Shanghai Chest Hospital, Shang... More >>hai, Shanghai, 200000, China\|Shanghai Pulmonary Hospital, Shanghai, Shanghai, 200000, China Less <<
NCT04636593	Non Small Cell Lung Cancer\|Sta... More >>ge III NSCLC\|EGFR Activating Mutation Less <<	PHASE2	UNKNOWN	2022-12-31	Hangzhou Cancer hospital, Hang... More >>zhou, Zhejiang, 310002, China Less <<
NCT06463171	Lung Cancer Non-small Cell Sta... More >>ge IV Less <<	PHASE2	NOT_YET_RECRUITING	2025-06-26	Zhongshan hospital, Shanghai, ... More >>200032, China\|The First Affiliated Hospital of Xiamen University, Xiamen, 361003, China Less <<
NCT04354961	Pulmonary Adenosquamous Carcin... More >>oma Less <<	PHASE2	RECRUITING	2025-06-30	Beijing Cancer Hospital, Beiji... More >>ng, China\|Beijing Chest Hospital, Capital Medical University, Beijing, China\|Cancer Hospital Chinese Academy of Medical Sciences, Beijing, China\|Hunan Cancer Hospital, Changsha, China\|The Second Xiangya Hospital of Central South University, Changsha, China\|Xinqiao Hospital, Army Medical University, Chongqing, China\|Fujian Cancer Hospital, Fuzhou, China\|Fujian Provincial Hospital, Fuzhou, China\|Sir Run Run Shaw Hospital, Hangzhou, China\|The second Affiliated Hospital of Kunming Medical University, Kunming, China\|The second Affiliated Hospital of Nanchang University, Nanchang, China\|Jiangsu Province Hospital, Nanjing, China\|Shanghai Chest Hospital, Shanghai, China\|Tianjin Medical University Cancer Institute & Hospital, Tianjin, China\|Tongji Hospital of Tongji Medical College,Huazhong University of Science and Technology, Wuhan, China\|Air Force Medical University of PLA (the Fourth Military Medical University), Xi'an, China\|Henan Cancer Hospital, Zhengzhou, China\|Henan Provincial People's Hospital, Zhengzhou, China Less <<
NCT06227897	Lung Cancer	PHASE2	WITHDRAWN	2029-04-01	Sun Yat-sen University Cancer ... More >>Center, Guangzhou, Guangdong, 510060, China Less <<
NCT04841811	Lung Cancer	PHASE3	RECRUITING	2026-12-31	Guangdong Lung cancer institut... More >>e, Guangzhou, Guangdong, 510080, China Less <<
NCT05662813	Non-small Cell Lung Cancer	PHASE2	RECRUITING	2025-06-30	West China Hospital，Sichuan Un... More >>iversity, Chendu, Sichuan, China Less <<
NCT05994339	Lung Cancer Stage III	PHASE2\|PHASE3	NOT_YET_RECRUITING	2025-12-08	-
NCT04882345	Lung Cancer\|EGFR Gene Mutation	PHASE2	UNKNOWN	2024-01-15	-
NCT05826483	Malignant Tumor of Lung\|Poor P... More >>erformance Status Less <<	PHASE1	RECRUITING	2024-12-30	Zhou Chengzhi, Guangzhou, Guan... More >>gdong, 510120, China Less <<
NCT05946460	Lung Cancer	PHASE2	RECRUITING	2025-07-10	The First Affiliated Hospital ... More >>of Guangzhou Medical University, Guangzhou, Guangdong, 510000, China Less <<
NCT02981108	Nonsmall Cell Lung Cancer	PHASE1\|PHASE2	UNKNOWN	2023-03-31	Pacific Cancer Medical Center,... More >> Inc., Anaheim, California, 92801, United States\|Beverly Hills Cancer Center, Beverly Hills, California, 90211, United States\|University of California San Diego Medical Center Moores Cancer Center, San Diego, California, 92093, United States\|University of Colorado-1775 Aurora Court, Aurora, Colorado, 80045, United States\|Sylvester Comprehensive Cancer Center, Deerfield Beach, Florida, 33442, United States\|University Cancer & Blood Center, LLC, Athens, Georgia, 30607, United States\|Baptist Healthcare Systems Inc. Baptist Health Floyd, New Albany, Indiana, 47150, United States\|Dartmouth-Hitchcock Medical Center, Hanover, New Hampshire, 03755, United States\|University of Texas Medical Branch at Galveston, Galveston, Texas, 77550, United States\|MultiCare Institute for Research and Innovation, Tacoma, Washington, 98405, United States Less <<
NCT04643847	EGFR Positive Non-small Cell L... More >>ung Cancer\|Brain Metastases Less <<	PHASE2	UNKNOWN	2023-11-30	Hangzhou Cancer Hospital, Hang... More >>zhou, Zhejiang, 310002, China Less <<
NCT04553887	Non Small Cell Lung Cancer	PHASE2	UNKNOWN	2023-05-01	Tianjin Medical University Can... More >>cer Institute and Hospital, Tianjin, Tianjin, China Less <<
NCT04808752	Lung Cancer	PHASE2	ACTIVE_NOT_RECRUITING	2024-07-15	Cancer Hospital Affiliated to ... More >>University of Chinese Academy of Sciences, Hangzhou, Zhejiang, 310000, China Less <<

Bio Calculators
Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	1.90mL 0.38mL 0.19mL	9.51mL 1.90mL 0.95mL	19.02mL 3.80mL 1.90mL
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