Structure of Poziotinib
CAS No.: 1092364-38-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
Synonyms: HM781-36B; NOV120101
4.5
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 1092364-38-9 |
Formula : | C23H21Cl2FN4O3 |
M.W : | 491.34 |
SMILES Code : | C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O |
Synonyms : |
HM781-36B; NOV120101
|
MDL No. : | MFCD28044290 |
InChI Key : | LPFWVDIFUFFKJU-UHFFFAOYSA-N |
Pubchem ID : | 25127713 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
A2780-SP cells | 20 nM | 6 days | Inhibited ovarian cancer stem cell sphere formation and viability, induced apoptosis | PMC7583017 |
SKOV3-SP cells | 10 nM | 6 days | Inhibited ovarian cancer stem cell sphere formation and viability, induced apoptosis | PMC7583017 |
MM134 HER2 L755S cells | 10 mM | 4 hours | To evaluate the inhibitory effect of poziotinib on downstream signaling in HER2 L755S cells, results showed that poziotinib significantly inhibited the expression of pHER2 and p-Akt. | PMC9379360 |
MCF7 L755S KI cells | 10 mM | 4 weeks | To evaluate the growth inhibitory effect of poziotinib on MCF7 L755S KI cells, results showed that poziotinib significantly inhibited cell growth. | PMC9379360 |
Ba/F3 cells | 1.0 nM | 72 hours | Poziotinib potently inhibited Ba/F3 cells with EGFR exon 20 mutations, with an IC50 value of 1.0 nM | PMC5964608 |
Ba/F3 cells | 1.9 nM | 72 hours | Poziotinib potently inhibited Ba/F3 cells with HER2 exon 20 mutations, with an IC50 value of 1.9 nM | PMC5964608 |
H1781 cells | 7.7 nM | 72 hours | Poziotinib potently inhibited H1781 cells, with an IC50 value of 7.7 nM | PMC5964608 |
CUTO14 cells | 1.84 nM | 72 hours | Poziotinib potently inhibited CUTO14 cells, with an IC50 value of 1.84 nM | PMC5964608 |
YUL-0019 cells | 0.30 nM | 72 hours | Poziotinib potently inhibited YUL-0019 cells, with an IC50 value of 0.30 nM | PMC5964608 |
SKOV3-SP cells | 10 nM | 6 days | Evaluate the effect of Manidipine alone or in combination with Poziotinib on the spheroid growth and viability of ovarian cancer stem cells. Results showed that combination treatment more effectively inhibited sphere size and viability than Manidipine alone. | PMC7583017 |
A2780-SP cells | 20 nM | 6 days | Evaluate the effect of Manidipine alone or in combination with Poziotinib on the spheroid growth and viability of ovarian cancer stem cells. Results showed that combination treatment more effectively inhibited sphere size and viability than Manidipine alone. | PMC7583017 |
SKOV3 cells | 10 nM | 6 days | Evaluate the effect of Manidipine alone or in combination with Poziotinib on the spheroid growth and viability of ovarian cancer stem cells. Results showed that combination treatment more effectively inhibited sphere size and viability than Manidipine alone. | PMC7583017 |
A2780 cells | 20 nM | 6 days | Evaluate the effect of Manidipine alone or in combination with Poziotinib on the spheroid growth and viability of ovarian cancer stem cells. Results showed that combination treatment more effectively inhibited sphere size and viability than Manidipine alone. | PMC7583017 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | MM134 HER2 L755S MIND xenograft model | Oral | 10 mg/kg | Once a week for 7 weeks | To evaluate the inhibitory effect of poziotinib on tumor growth and metastasis in the MM134 HER2 L755S MIND xenograft model, results showed that poziotinib significantly inhibited tumor growth and metastasis. | PMC9379360 |
Mice | EGFR D770insNPG genetically engineered mouse model | Oral | 10 mg/kg | daily for 4 weeks | Poziotinib significantly reduced tumor volume by 80% in GEMMs with an EGFR exon 20 mutation | PMC5964608 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03066206 | EGFR Exon 20 Mutation|ERBB2 Ge... More >>ne Mutation|Recurrent Lung Non-Small Cell Carcinoma|Stage IV Non-Small Cell Lung Cancer AJCC v7 Less << | PHASE2 | ACTIVE_NOT_RECRUITING | 2025-12-31 | M D Anderson Cancer Center, Ho... More >>uston, Texas, 77030, United States Less << |
NCT02216916 | HNSCC | PHASE2 | UNKNOWN | 2025-07-19 | Yonsei University, Seoul, Kore... More >>a, Republic of Less << |
NCT02544997 | Metastatic Breast Cancer | PHASE2 | COMPLETED | 2025-02-20 | Samsung Medical Center, Seoul,... More >> 135-710, Korea, Republic of Less << |
NCT02979821 | HER2 Gene Mutation|Adenocarcin... More >>oma Lung Stage IV Less << | PHASE2 | COMPLETED | 2025-12-17 | Korean Association for the Stu... More >>dy of Targeted Therapy, Seoul, Korea, Republic of Less << |
NCT04044170 | NSCLC | PHASE2 | TERMINATED | 2020-04-13 | Beijing Cancer Hospital, Beiji... More >>ng, China|Beijing Chest Hospital, Beijing, China|Beijing Hospital, Beijing, China|Cancer Hospital Chinese Academy of Medical Sciences, Beijing, China|Peking Union Medical College Hospital, Beijing, China|Jilin Cancer Hospital, Changchun, China|The First Hospital of Jilin University, Changchun, China|The Third Xiangya Hospital of Central South University, Changsha, China|Sichuan Cancer Hospital and Institute, Chengdu, China|West China Hospital of Sichuan University, Chengdu, China|Fujian Provincial Cancer Hospital, Fuzhou, China|Guangdong General Hospital, Guangzhou, China|Guangdong Panyu Central Hospital, Guangzhou, China|Shi Run Run Shaw Hospital, Zhejiang University, Hangzhou, China|The First Affiliated Hospital, Zhejiang University, Hangzhou, China|Zhejiang Cancer Hospital, Hangzhou, China|The Second Hospital of Anhui Medical University, Hefei, China|Shanghai Chest Hospital, Shanghai, China|University of Hong Kong-Shenzhen Hospital, Shenzhen, China|Cancer Center, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China|The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China|Chungbuk National University Hospital, Cheongju, Korea, Republic of|National Cancer Center, Gyeonggi-do, Korea, Republic of|Asan Medical Center, Seoul, Korea, Republic of|Samsung Medical Center, Seoul, Korea, Republic of|Seoul National University Hospital, Seoul, Korea, Republic of Less << |
NCT03318939 | NSCLC | PHASE2 | TERMINATED | 2023-04-03 | Mayo Clinic Hospital, Phoenix,... More >> Arizona, 85054, United States|Oncology Physician's Network Inc./OPN Healthcare, Arcadia, California, 91007, United States|City of Hope, Duarte, California, 91010, United States|UCSD -Moores Cancer Center, La Jolla, California, 92093, United States|Pacific Shores Medical Group, Long Beach, California, 90813, United States|Los Angeles Hematology Oncology Medical Group, Los Angeles, California, 90017, United States|USC/Norris Comprehensive Cancer Center, Los Angeles, California, 90033, United States|UC Davis Comprehensive Cancer Center, Sacramento, California, 95817, United States|UCSF Helen Diller Comprehensive Cancer Center at Mt Zion, San Francisco, California, 94115, United States|UCLA Hematology/Oncology, Santa Monica, California, 90404, United States|The Lundquist Institute for Biomedical Innovation at Harbor-UCLA Medical Center, Torrance, California, 90502, United States|Kaiser Permanente Medical Center, Vallejo, California, 94589, United States|Rocky Mountain Cancer Center, Boulder, Colorado, 80303, United States|Yale University, Yale Cancer Center Smilow Cancer Hospital at Yale, New Haven, Connecticut, 06510, United States|Georgetown University Medical Center, Washington, District of Columbia, 20007, United States|Florida Hospital, Orlando, Florida, 32804, United States|H. Lee Moffitt Cancer Center & Research Institute, Tampa, Florida, 33612, United States|The Bond & Steele Clinic, P.A. dba Bond Clinic, P.A., Winter Haven, Florida, 33881, United States|University Cancer & Blood Center, LLC, Athens, Georgia, 30607, United States|CTCA - Southeastern Regional Medical Center, Newnan, Georgia, 30265, United States|CTCA - Midwestern Regional Medical Center, Zion, Illinois, 60099, United States|Johns Hopkins Sidney Kimmel Comprehensive Cancer Center, Baltimore, Maryland, 21287, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Karmanos Cancer Institute, Detroit, Michigan, 48201, United States|Minnesota Oncology Hematology, P.A., Minneapolis, Minnesota, 55404, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|Hattiesburg Clinic Hematology/Oncology, Hattiesburg, Mississippi, 39401, United States|Montefiore Einstein Medical Center for Cancer Care, Bronx, New York, 10461, United States|North Shore Hematology Oncology Associates DBA New York Cancer and Blood Specialists, Bronx, New York, 10469, United States|Roswell Park Cancer Institute, Buffalo, New York, 14263, United States|NYU Langone Medical Center, New York, New York, 10016, United States|Weill Cornell Medical College, New York, New York, 10065, United States|North Shore Hematology Oncology Associates P.C. DBA NY Cancer and Blood Specialists, Port Jefferson Station, New York, 11776, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|Cleveland Clinic, Cleveland, Ohio, 44195, United States|The Ohio State University, Columbus, Ohio, 43210, United States|Oklahoma Cancer Specialists and Research Institute, LLC, Tulsa, Oklahoma, 74146, United States|CTCA - Eastern Regional Medical Center, Philadelphia, Pennsylvania, 19124, United States|Baptist Cancer Center, Memphis, Tennessee, 38120, United States|Texas Oncology- Austin, Austin, Texas, 78745, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Virginia Cancer Specialists, PC, Fairfax, Virginia, 22031, United States|Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|Saint Luc University Hospital, Brussels, Belgium|University Hospitals Leuven, Leuven, Belgium|Ambroise Pare University Hospital Center, Mons, Belgium|General Hospital Delta, Roeselare, Belgium|Cross Cancer Institute, Edmonton, Alberta, T6G 1Z2, Canada|BC Cancer - Vancouver, Vancouver, British Columbia, V5Z 4E6, Canada|London Regional Cancer Program, London, Ontario, N6A 5W9, Canada|Princess Margaret Cancer Centre, Toronto, Ontario, M5G 2M9, Canada|Hopital Larrey, CHU Toulouse, Unité d'Oncologie des Voies Respiratoires, Toulouse, France|Gustave Roussy Oncology Institute, Department of Medical Oncology, Villejuif, France|Soroka Medical Center, Be'er Sheva, Israel|Rambam Healthcare Campus, Haifa, Israel|Hadassah Medical Center, Jerusalem, Israel|Rabin Medical Center, Petah Tikva, Israel|National Cancer Institute, IRCCS, Department of Medical Oncology, Milan, Italy|Santa Maria delle Croci Hospital, Ravenna, Italy|National Cancer Institute Regina Elena, IRCCS, Operative Unit of Medical Oncology A 1, Rome, Italy|Erasmus Medical Center, Rotterdam, Netherlands|University Hospital Germans Trias i Pujol, Department of Medical Oncology, Barcelona, Spain|University Hospital 12 de Octubre, Madrid, Spain Less << |
NCT03744715 | NSCLC|Breast Cancer | PHASE2 | TERMINATED | 2023-03-03 | Pacific Shores Medical Group, ... More >>Long Beach, California, 90813, United States|Hattiesburg Clinic Hematology Oncology, Hattiesburg, Mississippi, 39401, United States|Laura and Isaac Perlmutter Cancer Center at NYU Langone, New York, New York, 10016, United States|UPMC, Pittsburgh, Pennsylvania, 15232, United States|UT MD Anderson Cancer Center, Houston, Texas, 77030, United States Less << |
NCT02659514 | Breast Cancer | PHASE2 | COMPLETED | 2020-03-11 | Clearview Cancer Center, Hunts... More >>ville, Alabama, 35805, United States|Pacific Cancer Medical Center, Inc., Anaheim, California, 92801, United States|Marin Cancer Care, Inc, Greenbrae, California, 94904, United States|Alliance Research Centers, Laguna Hills, California, 92653, United States|PacificShores Medical Group, Long Beach, California, 90813, United States|Valley Medical Oncology Consultants, Pleasanton, California, 94588, United States|Innovative Clinical Research Institute, Whittier, California, 90603, United States|AMPM Research Clinic, Miami Gardens, Florida, 33169, United States|FL Cancer Research Institute, Plantation, Florida, 33324, United States|Bond Clinic, P.A., Winter Haven, Florida, 33880, United States|Triple Army Medical Cente, Honolulu, Hawaii, 96859, United States|Franciscan St. Francis Health, Indianapolis, Indiana, 46237, United States|The University of Kansas Cancer Center and Medical Pavilion, Westwood, Kansas, 66205, United States|Hattiesburg Clinic Hematology Oncology, Hattiesburg, Mississippi, 39401, United States|Washington University, Saint Louis, Missouri, 63110, United States|St. Vincent Frontier Cancer Center, Billings, Montana, 59102, United States|North Shore Hematology Oncology Associates, East Setauket, New York, 11733, United States|Hudson Valley Hematology Oncology Associates, Poughkeepsie, New York, 12601, United States|White Plain Hospital, White Plains, New York, 10601, United States|Waverly Hematology Oncology, Cary, North Carolina, 27518, United States|Aultman Hospital, Canton, Ohio, 44710, United States|Ohio State University, Columbus, Ohio, 43210, United States|Oklahoma Cancer Specialists & Research Institute, LLC, Tulsa, Oklahoma, 74146, United States|Magee Womens Hospital of UPMC, Pittsburgh, Pennsylvania, 15213, United States|Charleston Cancer Center, Charleston, South Carolina, 29406, United States|Carolina Blood and Cancer Care Associates PA, Rock Hill, South Carolina, 29732, United States|Oncology Consultants, P.A., Houston, Texas, 77030, United States|SAMMC - Hem/Onc Clinic, Houston, Texas, 78234, United States|Texas Oncology-McAllen, McAllen, Texas, 78503, United States|The University of Texas Health Science Center at San Antonio, San Antonio, Texas, 78229, United States|Scott & White Memorial Hospital, Temple, Texas, 76508, United States|Providence Regional Cancer System, Lacey, Washington, 98503, United States|Medical Oncology Associates, PS, Spokane, Washington, 99208, United States|Northwest Medical Specialties, PLLC, Tacoma, Washington, 98405, United States|West Virginia University, Morgantown, West Virginia, 26506, United States Less << |
NCT01455571 | Advanced Solid Tumor | PHASE1 | COMPLETED | 2025-01-13 | Seoul National University Hosp... More >>ital, Seoul, Korea, Republic of Less << |
Tags: Poziotinib | NOV120101 | HM781-36B | UNII-OEI6OOU6IK | NOV-120101 | HM78136B | UNII OEI6OOU6IK |EGFR | Apoptosis | Epidermal growth factor receptor | ErbB-1 | HER1 | HER2 | HER-2 | HER-4 | pan-HER inhibitor | EGFR inhibitor | NSCLC | irreversible | ATP-competitive | tyrosine kinase inhibitor | TKI | 1092364-38-9
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H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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