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Chemical Structure| 1446261-44-4 Chemical Structure| 1446261-44-4

Structure of Pamiparib
CAS No.: 1446261-44-4

Chemical Structure| 1446261-44-4

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BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM.

Synonyms: BGB-290

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Product Details of Pamiparib

CAS No. :1446261-44-4
Formula : C16H15FN4O
M.W : 298.31
SMILES Code : O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51
Synonyms :
BGB-290
MDL No. :MFCD30489383

Safety of Pamiparib

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

Related Pathways of Pamiparib

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 0.02 - 200 nM 18 hours Pamiparib inhibits PARP activity in H2O2-treated HeLa cells with an IC50 of 0.24 nM PMC7350150
SW1990 cells 100 µM different time points Detected PD-L1 protein expression, found PD-L1 expression was up-regulated PMC8718453
BxPC-3 cells 100 µM different time points Detected PD-L1 protein expression, found PD-L1 expression was up-regulated PMC8718453
TNBC cells 60 mg 28 days Evaluate the antitumor effect of Pamiparib in TNBC cells, results showed a confirmed objective response rate (ORR) of 38.2% and a median progression-free survival (PFS) of 5.49 months. PMC9296104
HR+/HER2- cells 60 mg 28 days Evaluate the antitumor effect of Pamiparib in HR+/HER2- cells, results showed a confirmed objective response rate (ORR) of 61.9% and a median progression-free survival (PFS) of 9.20 months. PMC9296104
LN-229 cells 2.5 µM 120 hours Pamiparib did not increase cell death PMC8306656

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice BRCA1 mutated MDA-MB-436 breast cancer xenograft model oral 10 mg/kg three times/week for 3 weeks Pamiparib induced tumor regression on day 29 and resulted in 100% objective responses at the lowest dose (1.6 mg/kg) PMC7350150
nude mice SW1990 xenograft model oral 15 mg/kg Every 2-3 days for 19 days Detected PD-L1 expression, found PD-L1 expression was significantly up-regulated PMC8718453
Mouse Intracranial mIDH1 glioma model Intraperitoneal injection 1mg/mL 5 days per week for two weeks To evaluate the therapeutic effect of Pamiparib on mIDH1 glioma PMC10159884

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05327621 Metastatic Castration-resistan... More >>t Prostate Cancer Less << PHASE2 RECRUITING 2025-03-20 Sun Yat-sen University Cancer ... More >>Center, Guangzhou, Guangdong, 510060, China Less <<
NCT05489926 Epithelial Ovarian Cancer PHASE2 ACTIVE_NOT_RECRUITING 2025-12-24 Zhejiang Cancer Hospital, Hang... More >>zhou, Zhejiang, China Less <<
NCT03712930 Metastatic Castration-Resistan... More >>t Prostate Cancer (mCRPC)|Homologous Recombination Deficiency (HRD) Less << PHASE2 TERMINATED 2020-09-02 University Cancer and Blood Ce... More >>nter, Athens, Georgia, 30607, United States|Montefiore Einstein Cancer Center, Bronx, New York, 10461, United States|University of Washington, Seattle, Washington, 98195, United States|Gosford Hospital, Gosford, New South Wales, 2250, Australia|Liverpool Hospital, Liverpool, New South Wales, 2170, Australia|Calvary Mater Newcastle, Waratah, New South Wales, 2298, Australia|Icon Cancer Care Foundation, South Brisbane, Queensland, 044101, Australia|Pan American Oncology Trials, LLC, Rio Piedras, 935, Puerto Rico|L Hospitalet de Llobregat, Barcelona, 8035, Spain Less <<
NCT03575065 HER2-negative Breast Cancer PHASE2 COMPLETED 2021-04-14 Cancer Hospital Chinese Academ... More >>y of Medical Sciences, Beijing, Beijing, 100021, China|Fujian Medical University Union Hospital, Fuzhou, Fujian, 350001, China|Sun Yat Sen Memorial Hospital, Sun Yat Sen University (North), Guangzhou, Guangdong, 510000, China|Sun Yat Sen University Cancer Center, Guangzhou, Guangdong, 510060, China|Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, 150000, China|Henan Cancer Hospital, Zhengzhou, Henan, 450000, China|Zhongnan Hospital of Wuhan University Wuhan, Wuhan, Hubei, 430071, China|Xiangya Hospital of Central South University, Changsha, Hunan, 410008, China|Hunan Cancer Hospital, Changsha, Hunan, 410013, China|Jiangsu Province Cancer Hospital, Nanjing, Jiangsu, 210008, China|Jiangsu Province Hospital, Nanjing, Jiangsu, 210029, China|The First Hospital of Jilin University, Changchun, Jilin, 130021, China|The Second Hospital of Jilin University, Changchun, Jilin, 130022, China|Liaoning Cancer Hospital and Institute, Shenyang, Liaoning, 110042, China|Fudan University Shanghai Cancer Center, Shanghai, Shanghai, 200000, China|West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China|Sichuan Academy of Medical Sciences and Sichuan Provincial Peoples Hospital, Chengdu, Sichuan, 610071, China|Tianjin Medical University Cancer Institute and Hospital, Tianjin, Tianjin, 300060, China|Zhejiang University College of Medicine Second Affiliated Hospital, Hangzhou, Zhejiang, 310009, China|Zhejiang Cancer Hospital, Hangzhou, Zhejiang, 310022, China Less <<
NCT05483543 Limited Stage Small Cell Lung ... More >>Cancer Less << PHASE2 UNKNOWN 2024-12-31 Fudan University Shanghai Canc... More >>er Center, Shanghai, Shanghai, 200032, China|Fudan University Shanghai Cancer Center, Shanghai, Shanghai, 200032, China Less <<
NCT03333915 Advanced High-grade Ovarian Ca... More >>ncer|Triple Negative Breast Cancer Less << PHASE1|PHASE2 COMPLETED 2021-08-11 Cancer Hospital Chinese Academ... More >>y of Medical Sciences, Beijing, Beijing, 100021, China|Beijing Cancer Hospital, Beijing, Beijing, 100142, China|Henan Cancer Hospital, Zhengzhou, Henan, 450000, China|Hunan Cancer Hospital, Changsha, Hunan, 410013, China|Fudan University Shanghai Cancer Center, Shanghai, Shanghai, 200000, China|Zhejiang Cancer Hospital, Hangzhou, Zhejiang, 310022, China Less <<
NCT03933761 Ovarian Cancer|Carcinosarcoma PHASE2 WITHDRAWN 2021-08-02 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.76mL

3.35mL

1.68mL

33.52mL

6.70mL

3.35mL

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
 

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