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Chemical Structure| 1655504-04-3 Chemical Structure| 1655504-04-3

Structure of Orelabrutinib
CAS No.: 1655504-04-3

Chemical Structure| 1655504-04-3

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Orelabrutinib is an irreversible inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

Synonyms: ICP-022

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Product Details of Orelabrutinib

CAS No. :1655504-04-3
Formula : C26H25N3O3
M.W : 427.50
SMILES Code : O=C(C1=CC=C(C2CCN(C(C=C)=O)CC2)N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)N
Synonyms :
ICP-022
MDL No. :MFCD32184857
InChI Key :MZPVEMOYADUARK-UHFFFAOYSA-N
Pubchem ID :91667513

Safety of Orelabrutinib

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

Related Pathways of Orelabrutinib

RTK

Isoform Comparison

Biological Activity

Description
Orelabrutinib (ICP-022) acts as a potent, orally active, and irreversible inhibitor of Bruton's tyrosine kinase (BTK), exhibiting potential antineoplastic properties. It blocks the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-dependent activation of downstream survival pathways, thereby inhibiting the proliferation of malignant B-cells that overexpress BTK [1][2].

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04440059 Waldenstrom's Macroglobulinemi... More >>a Recurrent|Waldenstrom's Macroglobulinemia Refractory Less << PHASE2 COMPLETED 2024-01-09 The First Affiliated Hospital ... More >>of University of Science and Technology of China (Anhui Provincial Hospital), Hefei, Anhui, China|Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing, Beijing, 100000, China|West China hospital of sichuan university, Sichuan, Chengdu, China|Union Hospital affiliated to Fujian Medical University, Fuzhou, Fujian, China|The First Affiliated Hospital of Xiamen University, Xiamen, Fujian, China|First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, China|Henan Cancer Hospital, Zhengzhou, Henan, China|Henan Provincial Peoples's Hospital, Zhengzhou, Henan, China|Tongji Hospital affiliated to Huazhong University of Science and Technology, Wuhan, Hubei, China|Jiangsu Province Hospital, Nanjing, Jiangsu, China|The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, China|Shengjing Hospital of China Medical University, Shenyang, Liaoning, China|Ruijin Hospital affiliated to Shanghai Jiao Tong University, Shanghai, Shanghai, China|Hospital of Hematology, Chinese Academy of Medical Sciences, Tianjin, Tianjin, China|Union Hospital affiliated to Huazhong University of Science and Technology, Hubei, Wuhan, China|The First Affiliated Hospital of Zhejiang University Medical College, Hangzhou, Zhejiang, China Less <<
NCT05920668 CLL/SLL RECRUITING 2025-07-01 Department of Hematology, Shan... More >>dong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong, 250021, China Less <<
NCT03493217 CLL/SLL PHASE1|PHASE2 UNKNOWN 2022-12-31 Anhui Province Cancer Hospital... More >>, Hefei, Anhui, 230009, China|Peking University People's Hospital, Beijing, Beijing, 100044, China|Peking University Third Hospital, Beijing, Beijing, 100191, China|Peking Union Medical College Hospital, Beijing, Beijing, 100730, China|Fujian Medical University Union Hospital, Fuzhou, Fujian, 350001, China|The First Affiliated Hospital of Xiamen University, Xiamen, Fujian, 361003, China|Sun Yat-sen University Cancer Center, Guangzhou, Guangdong, 510060, China|Guangzhou First People's Hospital, Guangzhou, Guangdong, 510180, China|The Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei, 050011, China|Henan Provincial People's Hospital, Zhengzhou, Henan, 450003, China|Henan Tumor Hospital, Zhengzhou, Henan, 450008, China|Wuhan Union Hospital, Wuhan, Hubei, 430022, China|Tongji Hospital, Wuhan, Hubei, 430030, China|Jiangsu Province Hospital, Nanjing, Jiangsu, 210029, China|Jilin Cancer Hospital, Chang Chun, Jilin, 130012, China|The First Hospital of Jilin University, Changchun, Jilin, 130021, China|The second affiliated hospital of dalian medical university, Dalian, Liaoning, 116044, China|Qilu Hosptial of Shandong University, Jinan, Shandong, 250012, China|Shandong Provincial Hospital, Jinan, Shandong, 250021, China|Xinhua hospital affiliated to medical college of Shanghai jiao tong university, Shanghai, Shanghai, 200025, China|West China Hospital,Sichuan University, Chengdu, Sichuan, 610041, China|The Chinese Academy of Medical Sciences Hematology Hospital, Tianjin, Tianjin, 300020, China|Tianjin Medical University Cancer Institute and Hospital, Tianjin, Tianjin, 300060, China|The Second Affiliated Hospital Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310052, China|Second affiliated hospital of medical college of zhejiang university, Hangzhou, Zhejiang, China Less <<
NCT04438005 Diffuse Large B Cell Lymphoma PHASE2 COMPLETED 2021-12-13 Peking University Third Hospit... More >>al, Beijing, Beijing, 100191, China|Affiliated Tumor Hospital of Harbin Medical University, Haerbin, Heilongjiang, China|Jiangsu Province Hospital, Nanjing, Jiangsu, China|Shengjing Hospital of China Medical University, Shenyang, Liaoning, China|The Fourth Hospital of Hebei Medical University, Hebei, Shijiazhuang, China|Hematology Hospital of Chinese Academy of Medical Sciences (Institute of Hematology, Chinese Academy of Medical Sciences), Tianjin, Tianjin, China|The First Affiliated Hospital of Zhejiang University Medical College, Hangzhou, Zhejiang, 310000, China Less <<
NCT05284175 Neuromyelitis Optica Spectrum ... More >>Disorder Less << UNKNOWN 2025-08-23 Peking Union Medical College H... More >>ospital, Chinese Academy of Medical Sciences, Beijing, Beijing, 100730, China Less <<
NCT05334238 Primary Central Nervous System... More >> Lymphoma Less << PHASE3 RECRUITING 2025-05-30 Ruijin Hospital, Shanghai, Sha... More >>nghai, 20025, China Less <<
NCT05495828 B-cell Lymphoma RECRUITING 2025-03-10 Deparment of Hematology, Pekin... More >>g University People's Hospital, Beijing, Beijing, 100044, China Less <<
NCT05020288 Immune Thrombocytopenia|Bruton... More >>'s Tyrosine Kinase Less << PHASE2 UNKNOWN 2024-06-01 -
NCT06115824 Primary Central Nervous System... More >> Lymphoma Less << ACTIVE_NOT_RECRUITING 2024-09-30 Department of Hematology, Huas... More >>han Hospital, Fudan University, Shanghai, China Less <<
NCT06015464 Lymphoma, Large B-Cell, Diffus... More >>e Neoplasms by Histologic Type Less << NOT_YET_RECRUITING 2025-07-30 Hematological Department, Peop... More >>le's Hospital of Jiangsu Province, Nanjing, Jiangsu, 210029, China Less <<
NCT04438044 PCNSL|Secondary Central Nervou... More >>s System Lymphoma Less << PHASE2 UNKNOWN 2023-12-31 Beijing Cancer Hospital, Beiji... More >>ng, Beijing, China|Beijing Tiantan Hospital affiliated to Capital Medical University, Beijing, Beijing, China|Capital Medical University Xuanwu Hospital, Beijing, Beijing, China|Guangdong General Hospital, Guangzhou, Guangdong, China|Huashan Hospital affiliated to Fudan University, Shanghai, Shanghai, China Less <<
NCT03494179 Mantle Cell Lymphoma PHASE1|PHASE2 ACTIVE_NOT_RECRUITING 2023-12-31 Anhui Province Cancer Hospital... More >>, Hefei, Anhui, 230009, China|Peking University Third Hospital, Beijing, Beijing, 100191, China|Peking Union Medical College Hospital, Beijing, Beijing, 100730, China|Beijing Cancer Hospital, Beijing, Beijing, 102206, China|Fujian Medical University Union Hospital, Fuzhou, Fujian, 350001, China|The First Affiliated Hospital of Xiamen University, Xiamen, Fujian, 361003, China|Sun Yat-sen University Cancer Center, Guangzhou, Guangdong, 510060, China|Guangzhou First People's Hospital, Guangzhou, Guangdong, 510180, China|The Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei, 050011, China|Henan Provincial People's Hospital, Zhengzhou, Henan, 450003, China|Henan Tumor Hospital, Zhengzhou, Henan, 450008, China|The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, China|Wuhan Union Hospital, Wuhan, Hubei, 430022, China|Tongji Hospital, Wuhan, Hubei, 430030, China|Jiangsu Province Hospital, Nanjing, Jiangsu, 210029, China|Jilin Cancer Hospital, Chang Chun, Jilin, 130012, China|The First Hospital of Jilin University, Changchun, Jilin, 130021, China|The First Hospital of China Medical University, Shenyang, Liaojing, 110001, China|The Second Hospital of Dalian Medical University, Dalian, Liaoning, 116044, China|Liaoning Cancer Hospital and Institute, Shenyang, Liaoning, 110042, China|Qilu Hosptial of Shandong University, Jinan, Shandong, 250012, China|Shandong Provincial Hospital, Jinan, Shandong, 250021, China|The Affiliated Hospital of Qingdao University, Qingdao, Shandong, 266071, China|Zhongshan Hospital, Shanghai, Shanghai, 200032, China|Xin Hua Hospital Affiated to Shanghai Jiao Tong University School of Medicin, Shanghai, Shanghai, 200092, China|West China Hospital,Sichuan University, Chengdu, Sichuan, 610041, China|Tianjin Medical University Cancer Institute and Hospital, Tianjin, Tianjin, 300060, China|The First Affiliated Hospital of Zhengjiang University, Hangzhou, Zhejiang, 310003, China|Zhejiang Cancer Hospital, Hangzhou, Zhejiang, 310022, China|The Second Affiliated Hospital Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310052, China|The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, 325000, China Less <<
NCT05124028 Immune Thrombocytopenia PHASE1|PHASE2 UNKNOWN 2022-06-01 Peking University Institute of... More >> Hematology, Beijing, Beijing, 100044, China Less <<
NCT03797456 MZL PHASE2 COMPLETED 2024-02-06 Anhui Provincial Hospital, Hef... More >>ei, Anhui, 230002, China|Anhui Cancer Hospital, Hefei, Anhui, 230031, China|Chinese People's Liberation Army General Hospital Fifth Medical Center, Beijing, Beijing, 100039, China|Peking university People's Hospital, Beijing, Beijing, 100044, China|Beijing Cancer Hospital, Beijing, Beijing, 102206, China|Union Hospital Affiliated to Fujian Medical University, Fuzhou, Fujian, 350001, China|The Second Hospital of Lanzhou University, Lanzhou, Gansu, 730030, China|Sun Yat-sen University Cancer Center, Guangzhou, Guangdong, 510062, China|The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, Guangdong, 510120, China|Nanfang Hospital, Southern Medical University, Guangzhou, Guangdong, 510515, China|Guangdong Provincial People's Hospital, Guangzhou, Guangdong, 519041, China|Affiliated Hospital of Guizhou Medical University, Guiyang, Guizhou, 550004, China|The Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei, 050011, China|Affiliated Cancer Hospital of Harbin Medical University, Harbin, Heilongjiang, 150081, China|Henan Provincial People's Hospital, Zhengzhou, Henan, 450003, China|Henan Cancer Hospital, Zhengzhou, Henan, 450008, China|The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, China|Union Hospital Affiliated to Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, 430022, China|Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, 430030, China|Hunan Cancer Hospital, Changsha, Hunan, 410013, China|Jiangsu Provincial People's Hospital, Nanjing, Jiangsu, 210029, China|The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, 215006, China|Jiangxi Cancer Hospital, Nanchang, Jiangxi, 330029, China|First Hospital of Jilin University, Changchun, Jilin, 130061, China|Shandong Provincial Hospital, Jinan, Shandong, 250021, China|Qilu Hospital of Shandong University, Jinan, Shandong, 250063, China|Cancer Hospital Affiliated to Fudan University, Shanghai, Shanghai, 200032, China|West China Hospital of Sichuan University, Chengdu, Sichuan, 610044, China|Hematology Hospital, Chinese Academy of Medical Sciences, Tianjin, Tianjin, 300020, China|Tianjin Cancer Hospital, Tianjin, Tianjin, 300060, China|Zhejiang University Medical School affiliated to the first Hospital, Hangzhou, Zhejiang, 310003, China|Zhejiang Cancer Hospital, Hangzhou, Zhejiang, 310022, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL

Dissolving Methods
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

References

 

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