| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| ln Vitro |
PROTAC PARP2 degrader-1 (compound C8) (5-10 days of treatment) effectively inhibited the proliferation of MDA-MB-436, Capan-1, MDA-MB-468 and MDA-MB-231 cells, with IC50 values of 0.026 μM, 0.061 μM, 0.69 μM and 0.53 μM, respectively. In addition, its activity in non-BRCA mutant triple-negative breast cancer (TNBC) cells was significantly higher than that of olaparib [1]. PROTAC PARP2 degrader-1 (C8) (0.5 μM; 24 hours of treatment) selectively degraded PARP2 in the nucleus of MDA-MB-231 cells without affecting the level of cytoplasmic PARP2 [1]. PROTAC PARP2 degrader-1 (0.312-5 μM; 14 days of treatment) effectively and dose-dependently inhibited the colony formation of MDA-MB-231 cells [1]. PROTAC PARP2 degrader-1 (0.156–2.5 μM; 24–48 h) induced dose-dependent G2/M phase cell cycle arrest in MDA-MB-436 and MDA-MB-231 cells [1]. PROTAC PARP2 degrader-1 (C8) (0.312–5 μM; 48–72 h) induced dose-dependent apoptosis in MDA-MB-436 and MDA-MB-231 cells, and compared with olaparib [1].
|
|---|---|
| ln Vivo |
PROTAC PARP2 degrader-1 (compound C8) (12.5–100 mg/kg; ig, ip; 21 days) dose-dependently inhibited the growth of MDA-MB-231 TNBC xenografts [1].
|
| Cell Assay |
Immunofluorescence [1]
Cell Types: MDA-MB-231 (wild-type) triple-negative breast cancer cells Tested Concentrations: 0.5 μM Incubation Duration: 24 hours Experimental Results: The nuclear PARP2 was almost completely degraded, while the cytoplasmic PARP2 fluorescence remained unchanged. Compared with the inactive analogue C8-M, it had no effect on the PARP2 levels in both compartments. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female, 5-6 weeks old, subcutaneous xenograft model) [1]
Doses: 100 mg/kg (gavage); 12.5 mg/kg (intraperitoneal injection); 25 mg/kg (intraperitoneal injection) Route of Administration: Gavage; Intraperitoneal injection; Daily; 21 days Experimental Results: The tumor growth inhibition rate (TGI) in the 100 mg/kg gavage group was 63.5%. The tumor growth inhibition rate (TGI) in the 12.5 mg/kg intraperitoneal injection group was 82.9%. The tumor growth inhibition rate (TGI) in the 25 mg/kg intraperitoneal injection group was 98.3%. No significant weight loss, morbidity, or mortality was observed during the 21-day treatment period. No significant histopathological lesions were observed in the heart, liver, spleen, kidneys, and lungs after intraperitoneal injection of 25 mg/kg. |
| References |
| Molecular Formula |
C43H50CLFN6O6
|
|---|---|
| Molecular Weight |
801.35
|
| CAS # |
2925182-32-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1NN=C(CC2=CC=C(C(C(N3CCN(CC3)C(CCCCCCCCCNC(COC4=CC=C5C(CCCN5C(CCl)=O)=C4)=O)=O)=O)=C2)F)C6=C1C=CC=C6
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.2479 mL | 6.2395 mL | 12.4789 mL | |
| 5 mM | 0.2496 mL | 1.2479 mL | 2.4958 mL | |
| 10 mM | 0.1248 mL | 0.6239 mL | 1.2479 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
