DD-CIP2
Based on 1 Customer Validation
DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research.
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- Pureté: 99.72%
- Formule: C52H54ClFN10O5S
- Masse moléculaire:985.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
DD-CIP2 can target a broad spectrum of cancers with IC50 = 12 nM in Jurkat cell, IC50 = 12 nM in KARPASS422 cell, IC50 = 11 nM in Raji cell, IC50 = 2 nM in Daudi cell, IC50 = 9.3 nM in TYK-nu cell, and IC50 < 10 nM in MDA-MB-436, IC50 = 0.8 nM in SU-DHL-5 cells, IC50 = 4.6 nM in MOLT-4[1].
[1]
DD-CIP2 displays only a modest increase of PARP1 occupancy with EC50 = 42 nM[1].
DD-CIP2 (0.1-100 nM, 24 h) induces PARP1-BRD4 interaction in HEK293T cells and reduces DNA damage in both GLC16 and NCI-H82 cell lines[1].
DD-CIP2 (0.1-0.8 nM, 72 h) demonstrates the dependency on the PARP-170 BRD4 association in SU-DHL-5 cell[1].
DD-CIP2 (10 μM, 24 h) stalles cell cycle progression in GLC16 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:0.1, 1, 10 and 100 nM
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Incubation Time:24 h
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Result:Elevated levels of γH2AX and cleaved PARP1 in both GLC16 and NCI-H82 cell.
Increased the phosphorylation of RPA32 at Ser4/Ser8 in both GLC16 and NCI-H82 cell.
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Cell Line:GLC16 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Provoked a dose-dependent accumulation of 199 cells in the G2/M phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GLC16 cells (2 × 106, s.c.) induced NU-Foxn1nu mice (8 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p., once for 5 days
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Result:Induced a dose-dependent increase in γH2AX and cleaved PARP1, confirming target engagement.
Was well tolerated at doses up to 20 mg/kg, with no significant body weight loss.
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Animal Model:GLC16 cells (2 × 106, s.c.) induced NU-Foxn1nu mice (8 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p., once for 28 days
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Result:Showed strong tumor regression as early as day 3, with 210 durable suppression maintained throughout the experiment period.
Detected no obvious toxicity as indicated by steady body weight.
Chemical Information
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Appearance Solid
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Masse moléculaire 985.57
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Formule C52H54ClFN10O5S
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Color White to off-white
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SMILES
FC1=CC=C(CC2=NNC(C3=CC=CC=C32)=O)C=C1C(N(CC4)CCN4C(C(CC5)CCC65CCN(C(CNC(C[C@H]7C8=NN=C(C)N8C(SC(C)=C9C)=C9C(C%10=CC=C(Cl)C=C%10)=N7)=O)=O)CC6)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (101.46 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (2.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
Pureté et documentation
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Fiche technique (282 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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Instruction de manipulation (2659 KB)
Références
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 | 1.0146 mL | 5.0732 mL | 10.1464 mL | 25.3660 mL |
| 5 mM | 0.2029 mL | 1.0146 mL | 2.0293 mL | 5.0732 mL | |
| 10 mM | 0.1015 mL | 0.5073 mL | 1.0146 mL | 2.5366 mL | |
| 15 mM | 0.0676 mL | 0.3382 mL | 0.6764 mL | 1.6911 mL | |
| 20 mM | 0.0507 mL | 0.2537 mL | 0.5073 mL | 1.2683 mL | |
| 25 mM | 0.0406 mL | 0.2029 mL | 0.4059 mL | 1.0146 mL | |
| 30 mM | 0.0338 mL | 0.1691 mL | 0.3382 mL | 0.8455 mL | |
| 40 mM | 0.0254 mL | 0.1268 mL | 0.2537 mL | 0.6342 mL | |
| 50 mM | 0.0203 mL | 0.1015 mL | 0.2029 mL | 0.5073 mL | |
| 60 mM | 0.0169 mL | 0.0846 mL | 0.1691 mL | 0.4228 mL | |
| 80 mM | 0.0127 mL | 0.0634 mL | 0.1268 mL | 0.3171 mL | |
| 100 mM | 0.0101 mL | 0.0507 mL | 0.1015 mL | 0.2537 mL |