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Chemical Structure| 1557267-42-1 Chemical Structure| 1557267-42-1

Structure of Avitinib
CAS No.: 1557267-42-1

Chemical Structure| 1557267-42-1

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Avitinib selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate.

Synonyms: Abivertinib; AC0010

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Product Details of Avitinib

CAS No. :1557267-42-1
Formula : C26H26FN7O2
M.W : 487.53
SMILES Code : C=CC(NC1=CC=CC(OC2=C3C(NC=C3)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1)=O
Synonyms :
Abivertinib; AC0010
MDL No. :MFCD29089376
InChI Key :UOFYSRZSLXWIQB-UHFFFAOYSA-N
Pubchem ID :72734520

Safety of Avitinib

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

Related Pathways of Avitinib

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • mutant EGFR

    EGFR L858R/T790M, IC50:0.18 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
OCI-LY10 20 μM 24 hours Induce apoptosis in DLBCL cells PMC7052937
THP-1 1.25, 2.5, 5, and 10 μM 24 hours Evaluate the inhibitory effect of abivertinib and venetoclax on AML cell proliferation PMC7530784
KG-1a 1.25, 2.5, 5, and 10 μM 24 hours Evaluate the inhibitory effect of abivertinib and venetoclax on AML cell proliferation PMC7530784
MOLM-13 0.3125, 0.625, 1.25, and 2.5 μM 24 hours Evaluate the inhibitory effect of abivertinib and venetoclax on AML cell proliferation PMC7530784
MV4-11 0.3125, 0.625, 1.25, and 2.5 μM 24 hours Evaluate the inhibitory effect of abivertinib and venetoclax on AML cell proliferation PMC7530784
Rat liver microsomes (RLMs) 0, 1, 2.5, 5, 10, 25, 50, 100 μM 30 minutes To determine the inhibitory effect of Avitinib on CYP450 enzyme activity, results showed that Avitinib had varying degrees of inhibitory effects on cyp1a2, cyp2b1, cyp2d1, cyp2e1, and cyp3as. PMC8387736
Human liver microsomes (HLMs) 0, 1, 2.5, 5, 10, 25, 50, 100 μM 30 minutes To determine the inhibitory effect of Avitinib on CYP450 enzyme activity, results showed that Avitinib had varying degrees of inhibitory effects on CYP1A2, CYP2B6, CYP2D6, CYP2E1, and CYP3As. PMC8387736
Rat liver microsomes 1μM 50 minutes To evaluate the inhibitory effect of Avitinib on the metabolism of Osimertinib, with an IC50 value of 27.6 μM. PMC7529555

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice MV4-11-NSG xenograft model Oral 50 mg/kg Once daily for 18 days Evaluate the antileukemia effect of abivertinib and venetoclax combination therapy on AML xenograft model PMC7530784
Sprague-Dawley rats Healthy male Sprague-Dawley rats Oral 30 mg/kg Once daily for 7 days To evaluate the in vivo inhibitory effect of Avitinib on CYP450 enzyme activity, results showed that Avitinib significantly increased the AUC and Cmax of multiple probe substrates and decreased CLz/F and Vz/F, indicating that Avitinib inhibited the metabolic activity of CYP450 enzymes. PMC8387736
BALB/c nude mice DLBCL xenograft model Subcutaneous injection 30mg/kg Every 2 days for 10 days Inhibit tumor growth in DLBCL xenograft model PMC7052937

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03053219 Carcinoma,Non-Small-Cell Lung PHASE1 COMPLETED 2025-12-18 Jiangsu Province Hospital, Nan... More >>jing, Jiangsu, China Less <<
NCT03300115 Metastatic Non-small Cell Lung... More >> Cancer Less << PHASE2 UNKNOWN 2020-12-17 Beijing Cancer Hospital, Beiji... More >>ng, Beijing, 100000, China|Cancer Hospital Chinese Academy of Medical Sciences, Beijing, Beijing, 100000, China|Chinese PLA General Hospital, Beijing, Beijing, 100000, China|Daping Hospital,Research Institute of Surgery Third Military Medical University, Chongqing, Chongqing, 400000, China|Fujian Cancer Hospital, Fuzhou, Fujian, 350000, China|Guangdong Provincial People's Hospital, Guangzhou, Guangdong, 510000, China|The People's Hospital of Guangxi Zhuang Autonomous Region, Nanning, Guangxi, 530000, China|Henan Cancer Hospital, Zhengzhou, Henan, 450000, China|Tongji Medical College of HUST, Wuhan, Hubei, 430000, China|Zhongnan Hospital of Wuhan University, Wuhan, Hubei, 430000, China|The Third Xiangya Hospital of Central South University, Changsha, Hunan, 410000, China|Xiangya Hospital Central South University, Changsha, Hunan, 410000, China|The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, 215000, China|Northern Jiangsu People's Hospital, Yangzhou, Jiangsu, 225000, China|Jilin Cancer Hospital, Chang chun, Jilin, 130000, China|The First Hospital of Jilin University, Changchun, Jilin, 130000, China|Shandong Cancer Hospital, Jinan, Shandong, 250000, China|Tangdu Hospital, Xi'an, Shanxi, 710000, China|West China Hospital, Sichuan University, Chengdu, Sichuan, 610000, China|Tianjin Cancer Hospital, Tianjin, Tianjin, 300000, China|Tianjin Medical University General Hospital, Tianjin, Tianjin, 300000, China|Hangzhou First People's Hospital, Hangzhou, Zhejiang, 310000, China|Sir Run Run Shaw Hospital,Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310000, China|The Second Affiliated Hospital of Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310000, China|Zhejiang Cancer Hospital, Hangzhou, Zhejiang, 310000, China Less <<
NCT02274337 Non-Small Cell Lung Cancer PHASE1|PHASE2 UNKNOWN 2025-12-17 Sun Yat-Sen University Cancer ... More >>Center, Guangzhou, Guangdong, 510060, China Less <<
NCT03001609 Carcinoma, Non-Small-Cell Lung PHASE1 COMPLETED 2025-09-17 Jiangsu Province Hospital, Nan... More >>jing, Jiangsu, 210029, China Less <<
NCT02330367 Metastatic Non-small Cell Lung... More >> Cancer Less << PHASE1|PHASE2 UNKNOWN 2025-03-23 307 Hospital of PLA, Beijing, ... More >>Beijing, 100000, China|Beijing Cancer Hospital, Beijing, Beijing, 100000, China|Cancer Hospital Chinese Academy of Medical Sciences, Beijing, Beijing, 100000, China|Chinese PLA General Hospital, Beijing, Beijing, 100000, China|Peking Union Medical College Hospital, Beijing, Beijing, 100000, China|Fujian Medical University Union Hospital, Fuzhou, Fujian, 350000, China|Sun Yat-sen University Cancer Center, Guangzhou, Guangdong, 510000, China|Guangdong Provincial People's Hospital, Guangzhou, Guangdong, China|Hunan Cancer Hospital, Changsha, Hunan, 410000, China|Jiangsu Cancer Hospital, Nanjing, Jiangsu, 210000, China|Jiangsu Province Hospital, Nanjing, Jiangsu, 210000, China|Nanjing General Hospital of Nanjing Military Command, Nanjing, Jiangsu, 210000, China|Jilin Cancer Hospital, Chang Chun, Jilin, 130000, China|Shanghai Chest Hospital, Shanghai, Shanghai, 200000, China|West China Hospital,Sichuan University, Chendu, Sichuan, 610000, China|The First Affiliated Hospital, Zhejiang University, Hangzhou, Zhejiang, 310000, China|The Second Affiliated Hospital of Zhejiang University School of Medicine, Hanzhou, Zhejiang, 310000, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.51mL

4.10mL

2.05mL

References

 

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