Basroparib
Based on 1 Customer Validation
Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors.
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- 純度: 98.91%
- CAS 番号: 1858179-75-5
- 分子式: C18H21F2N7O3
- 分子量:421.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
PARP[1]
Basroparib (1.25-20 μM; 72 h) has synergistic inhibitory potency (CI <1) with the MEK inhibitor Trametinib (HY-10999) (3.125-50 nM; 72 h) in cell viability experiments of KRAS-G12V/D mutant colorectal cancer cell lines (such as SW480, SW620)[1].
Basroparib (5 μM; 14 d) significantly inhibits the colony formation of KRAS-G12V mutant cells (SW480, SW620), with enhanced inhibitory effect combined with Trametinib (5 nM; 14 d)[1].
Basroparib (5 μM; 7 d) inhibits the growth of 3D clonal spheroids of KRAS-G12V mutant cells, and significantly reduced the spheroid diameter combined with Trametinib (0.1 nM; 7 d)[1].
Basroparib (5 μM; 48 h) upregulates the AXIN1/2 protein level and downregulates the expression of phosphorylated β-catenin and p-ERK in KRAS-G12V mutant cells (SW480)[1].
Basroparib (5 μM; 48 h) reduces the nuclear active β-catenin aggregation in KRAS-G12V mutant cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480, SW620 (KRAS-G12V-mutated CRC)
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Concentration:1.25-20 μM; with or without 3.125-50 nM Trametinib
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Incubation Time:72 h
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Result:Combination treatment significantly reduced cell viability with synergistic effect (CI<1), particularly in KRAS-G12V/D-mutated cells compared to KRAS-G13D or wild-type cells.
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Cell Line:SW480 (KRAS-G12V-mutated CRC)
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Concentration:5 μM; with or without 10 nM Trametinib
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Incubation Time:48 h
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Result:Significantly reduced active β-catenin accumulation in the nucleus in cells treated with the combination, compared to vehicle or single-agent controls.
Basroparib (10 mg/kg; oral; once daily; for 4 weeks) combined with trametinib (0.5 mg/kg; oral; once daily), delays tumor regrowth in the trametinib-resistant SW620 tumor model in female nude mice and prolongs the survival of mice[1].
PK parameters of Basroparib[2]
| Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | AUC0-t (ng·h/mL) | T1/2 (h) | Relative | Bioavailability |
| p.o. | 10 | 1021 | 1 | 5458 | 5.39 | 1 | / |
| p.o. | 1 | 95 | 1 | 244 | 4.26 | 1 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (4 weeks old) with KRAS-G12V-mutated CRC xenograft model[1]
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Dosage:10 mg/kg with or without 0.5 mg/kg Trametinib (oral suspension)
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Administration:Oral gavage, once daily, 17-28 days (while 27 days for SW620, 26 days for DLD-1, 17 days for COLO320DM, and 28 days for SW480)
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Result:Combination treatment resulted in 87.2% tumor growth inhibition (TGI) in SW620 xenografts, with reduced nuclear β-catenin and p-ERK levels in tumor tissues compared to single agents. No significant body weight loss was observed.
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Animal Model:Female nude mice (4 weeks old) with Trametinib-resistant SW620 (KRAS-G12V-mutated CRC) xenograft model[1]
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Dosage:10 mg/kg with or without 0.5 mg/kg Trametinib (oral suspension)
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Administration:Oral gavage, once daily, 4 weeks
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Result:Combination treatment suppressed tumor regrowth (TGI=66.9%) and increased survival rate (median survival >90 days vs. 60 days in trametinib alone group).
Immunoblotting showed reduced Wnt pathway activation (lower active β-catenin and EpCAM) in tumor tissues.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1858179-75-5
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性状 Solid
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分子量 421.40
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分子式 C18H21F2N7O3
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Color White to light yellow
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SMILES
O=C1N=C(N2CCN(CC2)C3=C(C=C(C=C3F)OCCOC)F)NC4=C1N=NN4C
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別名
STP1002
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (237.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (254 KB)
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- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kwon YJ, et al. Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer. Biochem Pharmacol. 2025 May;235:116842. [Content Brief]
[3]. Bai YR, et al. The recent advance and prospect of poly(ADP-ribose) polymerase inhibitors for the treatment of cancer. Med Res Rev. 2024 Aug 24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3730 mL | 11.8652 mL | 23.7304 mL | 59.3261 mL |
| 5 mM | 0.4746 mL | 2.3730 mL | 4.7461 mL | 11.8652 mL | |
| 10 mM | 0.2373 mL | 1.1865 mL | 2.3730 mL | 5.9326 mL | |
| 15 mM | 0.1582 mL | 0.7910 mL | 1.5820 mL | 3.9551 mL | |
| 20 mM | 0.1187 mL | 0.5933 mL | 1.1865 mL | 2.9663 mL | |
| 25 mM | 0.0949 mL | 0.4746 mL | 0.9492 mL | 2.3730 mL | |
| 30 mM | 0.0791 mL | 0.3955 mL | 0.7910 mL | 1.9775 mL | |
| 40 mM | 0.0593 mL | 0.2966 mL | 0.5933 mL | 1.4832 mL | |
| 50 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1865 mL | |
| 60 mM | 0.0396 mL | 0.1978 mL | 0.3955 mL | 0.9888 mL | |
| 80 mM | 0.0297 mL | 0.1483 mL | 0.2966 mL | 0.7416 mL | |
| 100 mM | 0.0237 mL | 0.1187 mL | 0.2373 mL | 0.5933 mL |
Basroparib 関連分類
HY-147245 関連分類
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