| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Basroparib potently targets tankyrase 1 (TNKS1) with an IC50 of 29.94 nM and tankyrase 2 (TNKS2) with an IC50 of 3.68 nM. It demonstrates excellent selectivity, exhibiting very limited activity against PARP1 (IC50 >10 uM) and does not significantly inhibit a broad panel of other human kinases or receptors.
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| ln Vitro |
In cell-free enzymatic assays, Basroparib inhibits TNKS1/2 with high potency. In APC-mutated colorectal cancer (CRC) cell lines, it stabilizes AXIN1/2 proteins, effectively disrupts the Wnt/beta-catenin signaling pathway (IC50=8.3 nM), and inhibits cell proliferation. It also resensitizes KRAS-mutant CRC cells to MEK inhibitors.
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| ln Vivo |
In mouse xenograft models of APC-mutated CRC, oral administration of Basroparib at 10-30 mg/kg once daily (QD) significantly inhibits tumor growth in a dose-dependent manner. It does not show significant on-target gastrointestinal tract toxicity in vivo compared to other tankyrase inhibitors.
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| Enzyme Assay |
For cell-free kinase assays, purified recombinant TNKS2 (0.5 nM) is incubated with 25 uM biotinylated-NAD+ and varying concentrations of Basroparib (0.01-1000 nM) in assay buffer for 90 minutes. PARsylation activity is detected by AlphaScreen or ELISA. IC50 values are calculated from dose-response curves.
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| Cell Assay |
APC-mutated CRC cells (e.g., HCT116 or HT29) are seeded and treated with serial dilutions of Basroparib (1 nM-10 uM). After 72-96 hours, cell viability is assessed using CellTiter-Glo. Wnt/beta-catenin activity is evaluated by TOPFlash/FOPFlash luciferase reporter assays. Apoptosis is measured by caspase-3/7 activity and Annexin V staining.
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| Animal Protocol |
Female BALB/c nude mice bearing subcutaneous APC-mutated CRC xenografts (e.g., HCT116) are treated with Basroparib at doses of 10, 20, or 30 mg/kg by oral gavage once daily for 21-28 days. Tumor volume is measured bi-weekly, and tumors are harvested at the study endpoint for assessment of AXIN stabilization and Wnt target gene expression.
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| ADME/Pharmacokinetics |
Basroparib is orally bioavailable. Following a single oral dose of 10 mg/kg in rats, it has a terminal half-life (t½) of approximately 2.5 hours, a moderate clearance (CL) of 45 mL/min/kg, and a volume of distribution (Vd) of 9.7 L/kg. The compound shows good in vivo exposure and stability, with a half-life supporting once-daily dosing.
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| Toxicity/Toxicokinetics |
In preclinical studies, Basroparib shows no significant on-target toxicity in the gastrointestinal tract, a known issue for some tankyrase inhibitors. Standard safety precautions for research chemicals apply. It is for research use only, not for human consumption.
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| References | |
| Additional Infomation |
Basroparib is an orally bioavailable poly(ADP-ribose) polymerase (PARP) tankyrase inhibitor with potential antitumor activity. After administration, basroparib selectively binds to and inhibits tankyrase activity. This may block the polymerization (ADP-ribose) of multiple target proteins, including various tumor suppressor factors, mediated by tankyrase. This may include blocking the polymerization (ADP-ribose) and destabilization of the β-catenin negative regulator AXIN, thereby inhibiting the Wnt/β-catenin signaling pathway. This may inhibit the transcriptional activation of multiple target genes in the Wnt/β-catenin signaling pathway, thereby suppressing the gene expression of many Wnt-related pro-survival proteins and inhibiting tumor cell growth. Tankyrase is a member of the PARP family and plays an important role in the Wnt/β-catenin signaling pathway, tumor suppressor factors, and telomere maintenance and mitotic regulation.
Basroparib is also known as STP1002. It has undergone a Phase 1, first-in-human clinical trial (NCT04505839) in patients with advanced solid tumors. The INN stem "-parib" indicates it is a PARP enzyme inhibitor. Purity: ≥98%. Chemical formula: C18H21F2N7O3; molecular weight: 421.40. Store at -20degC. |
| Molecular Formula |
C18H21F2N7O3
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|---|---|
| Molecular Weight |
421.401249647141
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| Exact Mass |
421.167
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| Elemental Analysis |
C, 51.30; H, 5.02; F, 9.02; N, 23.27; O, 11.39
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| CAS # |
1858179-75-5
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| PubChem CID |
137017382
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
637
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(N2CCN(C3=C(F)C=C(OCCOC)C=C3F)CC2)NC(=O)C2N=NN(C)C=2N=1
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| InChi Key |
ALDDPEMJJONRDI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21F2N7O3/c1-25-16-14(23-24-25)17(28)22-18(21-16)27-5-3-26(4-6-27)15-12(19)9-11(10-13(15)20)30-8-7-29-2/h9-10H,3-8H2,1-2H3,(H,21,22,28)
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| Chemical Name |
5-[4-[2,6-difluoro-4-(2-methoxyethoxy)phenyl]piperazin-1-yl]-3-methyl-6H-triazolo[4,5-d]pyrimidin-7-one
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| Synonyms |
Basroparib; STP-1002; STP 1002; 1858179-75-5; Basroparib [INN]; P5LYN8CD74; STP1002;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (237.3 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3730 mL | 11.8652 mL | 23.7304 mL | |
| 5 mM | 0.4746 mL | 2.3730 mL | 4.7461 mL | |
| 10 mM | 0.2373 mL | 1.1865 mL | 2.3730 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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