Pamiparib (BGB-290)
(Synonyms: 帕米帕利,BGB-290) 目录号 : GC34071
Pamiparib (BGB-290)是一种强效口服的聚腺苷二磷酸核糖聚合酶（PARP）抑制剂，对PARP-1和PARP-2的IC50值分别为1.3nM和0.9nM。
Cas No.:1446261-44-4
Sample solution is provided at 25 µL, 10mM.
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Pamiparib (BGB-290) is a potent and oral Poly (ADP-ribose) polymerase (PARP) inhibitor, with IC50 values of 1.3nM and 0.9nM for PARP-1 and PARP-2, respectively [1]. Pamiparib has excellent bioavailability and exhibits high cytotoxicity and potent DNA-trapping activity (with an IC50 of 13nM)[2]. Pamiparib has been widely used as an anti-cancer agent in both cancer cells and xenograft (PDX) models[3].
In vitro, Pamiparib treatment for 7 days significantly inhibited MDA-MB-436 cells and UWB1.289 cells, with IC50 values of 41±15nM and 54nM, respectively[4]. Treatment of OCI-Ly3 cells with 25µM Pamiparib for 24 hours promoted doxorubicin-induced cell apoptosis and reversed the chemoresistance associated with miRNA-363-3p[5]. The 10μM dose of Pamiparib treatment for 14 days significantly inhibited the colony formation of Fh1-deficient RENCA cells[6].
In, vivo, Pamiparib treatment via oral administration at 3mg/kg twice daily for 3 weeks significantly inhibited tumor growth in mice with SW1990 cell xenografts and reduced the number of Ki-67-positive tumor cells[7]. A single oral administration of 3mg/kg Pamiparib for 4 hours inhibited PARylation in the brain and tumor tissues of the intracranial H209 cell xenograft tumor mouse model, and the survival period of the mice was significantly prolonged[8].
References:
[1] Wang H, Ren B, Liu Y, et al. Discovery of pamiparib (BGB-290), a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor in clinical development[J]. Journal of Medicinal Chemistry, 2020, 63(24): 15541-15563.
[2] Tang Z, Liu Y, Zhen Q, et al. BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models[J]. Cancer Research, 2015, 75(15_Supplement): 1653-1653.
[3] Gupta S K, Mladek A C, Jain S, et al. Pamiparib-induced replication stress augments the efficacy of temozolomide in GBM PDX models[J]. Cancer Research, 2025, 85(8_Supplement_1): 2910-2910.
[4] Xiong Y, Guo Y, Liu Y, et al. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor[J]. Neoplasia, 2020, 22(9): 431-440.
[5] Zhou W, Xu Y, Zhang J, et al. MiRNA-363-3p/DUSP10/JNK axis mediates chemoresistance by enhancing DNA damage repair in diffuse large B-cell lymphoma[J]. Leukemia, 2022, 36(7): 1861-1869.
[6] Ueno D, Vasquez J C, Sule A, et al. Targeting Krebs-cycle-deficient renal cell carcinoma with Poly ADP-ribose polymerase inhibitors and low-dose alkylating chemotherapy[J]. Oncotarget, 2022, 13: 1054.
[7] Wang Y, Zheng K, Xiong H, et al. PARP inhibitor upregulates PD-L1 expression and provides a new combination therapy in pancreatic cancer[J]. Frontiers in immunology, 2021, 12: 762989.
[8] Tang Z, Jiang B, Shi Z, et al. BGB-290, a novel PARP inhibitor with unique brain penetration ability, demonstrated strong synergism with temozolomide in subcutaneous and intracranial xenograft models[J]. Cancer Research, 2015, 75(15_Supplement): 1651-1651.
Pamiparib (BGB-290)是一种强效口服的聚腺苷二磷酸核糖聚合酶（PARP）抑制剂，对PARP-1和PARP-2的IC50值分别为1.3nM和0.9nM[1]。Pamiparib具有优异的生物利用度，表现出高细胞毒性和强效DNA捕获活性（IC50=13nM）[2]。Pamiparib已广泛应用于癌细胞和异种移植（PDX）模型的抗癌研究[3]。
在体外，Pamiparib处理7天可显著抑制MDA-MB-436和UWB1.289细胞，IC50值分别为41±15nM和54nM[4]。25µM的Pamiparib处理OCI-Ly3细胞24小时能促进多柔比星诱导的细胞凋亡，并逆转与miRNA-363-3p相关的化疗耐药性[5]。10µM的Pamiparib处理Fh1缺陷型RENCA细胞14天可显著抑制克隆细胞形成[6]。
在体内，SW1990细胞异种移植小鼠每日两次口服Pamiparib（3mg/kg；持续3周）可显著抑制肿瘤生长并减少Ki-67阳性肿瘤细胞数量[7]。颅内H209细胞异种移植瘤小鼠单次口服3mg/kg剂量的Pamiparib（4小时）能抑制脑组织和肿瘤中的PAR化修饰，并显著延长生存期[8]。
| Cell experiment [1]: | |
Cell lines | HeLa cells |
Preparation Method | HeLa cells were inoculated into 96-well plates (with transparent bottoms and black walls) at an initial concentration of 5×103 cells per well, and the culture medium was 100μL DMEM (containing 10% FBS, 0.1mg/mL penicillin-streptomycin). After 4 hours, Pamiparib was added to the cell culture medium with the different concentration (0.001, 0.01, 0.1, 1, 10, 100, 1000, and 10000nM), and the DMSO/culture medium ratio was 0.1%. After the Pamiparib treatment for 18 hours, 200μM H2O2 solution was used to induce DNA damage at 37°C for 5 minutes. The cells were further fixed in 100μL/well cold methanol at -20°C for 20 minutes. After fixation and brief washing, the cells were stained in the detection buffer [50μL/well, containing PBS, Tween (0.1%) and BSA (1mg/mL)], and the buffer contained a primary antibody PAR mAb (1:2000), a secondary antibody Alexa Fluor 488 antibody (1:2000), which was incubated at 4°C in the dark overnight. The PAR signal of the cells was analyzed. |
Reaction Conditions | 0.001, 0.01, 0.1, 1, 10, 100, 1000, and 10000nM; 18h |
Applications | Pamiparib treatment significantly inhibited intracellular PAR levels in H2O2-treated HeLa cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6 mice |
Preparation Method | Female C57BL/6 mice (6 weeks old) were raised under standard laboratory conditions and were fed with sterile food and water. 100μl of SW1990 cell suspension was injected into the right lumbar region of each mouse (i.e., the injection volume was 2×106). When the tumor volume of the mice exceeded 100mm3 [tumor volume = (length × width × width)/2], the mice were divided into the Pamiparib experimental group and the control group. The mice in the Pamiparib experimental group were orally administered Pamiparib (3mg/kg) twice daily, and the mice in the control group received no special treatment. After 3 weeks of administration, the mice were sacrificed, and the tumor tissues were extracted, labeled, and fixed with 4% paraformaldehyde for analysis. |
Dosage form | 3mg/kg twice daily for 3 weeks; p.o. |
Applications | Pamiparib treatment significantly inhibited tumor growth in mice and reduced the number of Ki-67-positive tumor cells. |
References: | |
| Cas No. | 1446261-44-4 | SDF | |
| 别名 | 帕米帕利,BGB-290 | ||
| Canonical SMILES | O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51 | ||
| 分子式 | C16H15FN4O | 分子量 | 298.31 |
| 溶解度 | DMSO : 83.3 mg/mL (279.24 mM) | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3522 mL | 16.7611 mL | 33.5222 mL |
| 5 mM | 670.4 μL | 3.3522 mL | 6.7044 mL |
| 10 mM | 335.2 μL | 1.6761 mL | 3.3522 mL |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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