| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
PARP1 PROTAC 180055 (1-10 μM, 24-48 h) can protect T47D and MOLT4 cells from genotoxic-induced cell death [1]. PARP1 PROTAC 180055 (10 μM, 3-6 days) can produce significant cytotoxic effects on MOLT4 cells carrying BRCA1 mutations [1].
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|---|---|
| ln Vivo |
PARP1 PROTAC 180055 (40 mg/kg, intraperitoneal injection, 16 days) showed antitumor activity in BRCA1-mutant MOLT4 xenograft mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: BRCA1-free cardiomyocyte cell lines and MOLT4 cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 144 hours Experimental Results: Showed very low cytotoxicity to BRCA1-free cardiomyocyte cell lines. Induced significant cytotoxicity in MOLT4 cells carrying the BRCA1 mutation. |
| Animal Protocol |
Animal/Disease Models:5-week-old NSG mice (injected with 8 × 10⁶ MOLT4 cells or 4 × 10⁶ A2780 cells) [1]
Doses: 40 mg/kg Route of Administration: Intraperitoneal injection (ip) for 16 days Experimental Results: Tumor volume was significantly reduced compared to the control group. PARP1 in MOLT4 xenografted mouse tumors was effectively degraded. No significant changes were observed in neutrophil count, lymphocyte count, or alanine aminotransferase levels. |
| References |
| Molecular Formula |
C51H62FN7O6S
|
|---|---|
| Molecular Weight |
920.14
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| Appearance |
Light yellow to yellow solid
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| SMILES |
O=C1NCCC2=C(C3=CC=C(CN(C)C(CCCCCCCCC(N[C@H](C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)C(C)(C)C)=O)=O)C=C3)NC7=CC(F)=CC1=C72
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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 Note: 本产品在运输和储存过程中需避光（避免光照）。 |
| 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 (~108.68 mM; with sonication)
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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 | 1.0868 mL | 5.4340 mL | 10.8679 mL | |
| 5 mM | 0.2174 mL | 1.0868 mL | 2.1736 mL | |
| 10 mM | 0.1087 mL | 0.5434 mL | 1.0868 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.
Products are for research use only; We do not sell to patients
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