TDI-012804
Based on 1 Customer Validation
TDI-012804 is a TNKS2 inhibitor that inhibits the PARP catalytic domain activity of TNKS1/TNKS2. TDI-012804 stabilizes AXIN1 and inhibits WNT signaling. TDI-012804 reduces colony formation and proliferation of TNKS1-deficient cancer cell lines and APC-mutant intestinal organoids, whereas TNKS1 wild-type organoids show lower sensitivity. TDI-012804 can be used in research related to colorectal cancer.
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- Purity : 99.53%
- CAS No.: 3120102-92-0
- 화학식: C30H26N4O4
- 분자량:506.55
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
TDI-012804 (24 h) stabilizes AXIN1 with greater potency in TNKS1-knockdown NIH3T3 cells (EC50 54.7 nM) than in TNKS1WT cells (EC50 221.9 nM)[1].
TDI-012804 (48 h) inhibits WNT-mediated transcription in DLD1 cells with an EC50 <100 nM and shows higher sensitivity in TNKS1HET cells[1].
TDI-012804 (250-500 nM; 24 h) selectively stabilizes endogenous AXIN1 in TNKS1HET and TNKS1KO DLD1 cells[1].
TDI-012804 (24 h)-induced AXIN1 stabilization in DLD1 cells requires a TNKS2 L1136-sensitive B-loop conformation[1].
TDI-012804 (16 days) preferentially inhibits colony formation in TNKS1-deficient or 8p-heterozygous cancer cells[1].
TDI-012804 (500 nM; 3 days) selectively alters the WNT-dependent transcriptome in ApcQ1405X/Tnks1KO organoids, with no significant transcriptional effect on Tnks1WT organoids[1].
TDI-012804 (6-20 days) selectively inhibits the proliferation of ApcQ1405X/Tnks1KO organoids with an EC50 of 59.1 nM, whereas Tnks1WT organoids are 19-fold less sensitive[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD1 TNKS1WT, TNKS1HET, and TNKS1KO cells
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Concentration:250 and 500 nM
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Incubation Time:24 h
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Result:Induced marked stabilization of endogenous AXIN1 in TNKS1HET and TNKS1KO DLD1 cells but induced only a minimal increase in AXIN1 protein in TNKS1 diploid controls.
Chemical Information
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CAS No. 3120102-92-0
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Appearance Solid
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분자량 506.55
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화학식 C30H26N4O4
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Color Light yellow to light brown
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SMILES
COC1=C(C(NC2=CC=C(C(NC(C3=CC=C(C(O)(C)C)C=C3)=N4)=O)C4=C2)=O)C=NC(C5=CC=CC=C5)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
DMSO : 100 mg/mL (197.41 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.94 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 | 1.9741 mL | 9.8707 mL | 19.7414 mL | 49.3535 mL |
| 5 mM | 0.3948 mL | 1.9741 mL | 3.9483 mL | 9.8707 mL | |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9741 mL | 4.9353 mL | |
| 15 mM | 0.1316 mL | 0.6580 mL | 1.3161 mL | 3.2902 mL | |
| 20 mM | 0.0987 mL | 0.4935 mL | 0.9871 mL | 2.4677 mL | |
| 25 mM | 0.0790 mL | 0.3948 mL | 0.7897 mL | 1.9741 mL | |
| 30 mM | 0.0658 mL | 0.3290 mL | 0.6580 mL | 1.6451 mL | |
| 40 mM | 0.0494 mL | 0.2468 mL | 0.4935 mL | 1.2338 mL | |
| 50 mM | 0.0395 mL | 0.1974 mL | 0.3948 mL | 0.9871 mL | |
| 60 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8226 mL | |
| 80 mM | 0.0247 mL | 0.1234 mL | 0.2468 mL | 0.6169 mL | |
| 100 mM | 0.0197 mL | 0.0987 mL | 0.1974 mL | 0.4935 mL |
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