QC-182
Based on 1 Customer Validation
QC-182 is a p300/CBP PROTAC degrader with a DC50 of 93 nM against p300. QC-182 induces ubiquitination and proteasomal degradation of p300 and CBP in a CRBN-dependent manner. QC-182 induces Apoptosis. QC-182 exhibits anticancer activity against liver cancer cells. QC-182 can be used for the research of hepatocellular carcinoma.
(Pink: CBP/p300 ligand (HY-175907); Blue: Cereblon ligand (HY-14658); Black: linker (HY-40146)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.94%
- CAS No.: 3032646-96-8
- Formule: C44H42F2N8O6
- Masse moléculaire:816.85
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform PROTACs
More
Activité biologique
|
p300 93 nM (DC50) |
Cereblon |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SK-HEP1 | IC50 |
0.733 μM
Compound: 19; QC-182
|
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
|
[PMID: 38316017] |
QC-182 (10-1000 nM; 0.5-24 h) potently induces dose- and time-dependent degradation of p300 (DC50 = 93 nM) and CBP in SK-HEP-1 cells via the CRBN-dependent ubiquitin-proteasome pathway[1].
QC-182 (0-100 μM; 5 days) potently inhibits the proliferation of hepatocellular carcinoma cells SK-HEP-1 (IC50 = 0.733 μM) and JHH-7 (IC50 = 0.447 μM)[1].
QC-182 (0.5-2 μM; 14 days) effectively inhibits colony formation of hepatocellular carcinoma cell line SK-HEP-1 in a dose-dependent manner[1].
QC-182 (0.5-2 μM; 72 h for apoptosis assays) induces dose-dependent G2/M cell cycle arrest and apoptosis in hepatocellular carcinoma SK-HEP-1 cells, a process associated with downregulated expression of CDK6 and SKP2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SK-HEP-1 human hepatocellular carcinoma cells
-
Concentration:0.01 μM, 0.1 μM, 1 μM, 10 nM, 100 nM, 250 nM, 500 nM, 1000 nM, 0.5 μM, 2 μM; 0.5 μM (with 1 μM MG132 pretreatment); 0.5 μM (with 0.1 μM, 0.5 μM MLN4924 pretreatment); 1 μM (with 0.5 μM thalidomide pretreatment); 1 μM (in CRBN-knockdown cells); 2 μM (with 1 μM MG132 pretreatment)
-
Incubation Time:24 h; 0.5 h, 1 h, 6 h, 12 h, 24 h (1 μM treatment)
-
Result:Degraded 9% of p300 at 0.01 μM, 27% at 0.1 μM, and 47% at 1 μM after 24 h treatment.
Reduced p300 levels in a dose-dependent manner with a DC50 of 93 nM, with no hook effect up to 1000 nM.
Initiated p300 degradation at 1 h after treatment with 1 μM QC-182, reaching sustained reduction by 6 h.
Degraded CBP in a dose-dependent manner, reducing levels by 2% at 0.5 μM, 8% at 1 μM, and 11% at 2 μM after 24 h.
Had its induced p300 degradation blocked by pretreatment with MG132, MLN4924, or thalidomide, as well as by CRBN knockdown.
Increased p300 ubiquitination compared to vehicle or parental inhibitor QC-124.
-
Cell Line:SK-HEP-1 and JHH-7 human hepatocellular carcinoma cells
-
Concentration:0-100 μM
-
Incubation Time:5 days
-
Result:Potently inhibited cell growth in SK-HEP-1 cells with an IC50 of 0.733 μM.
Potently inhibited cell growth in JHH-7 cells with an IC50 of 0.447 μM.
Exhibited superior potency compared to parental inhibitors CCS1477 and QC-124, and reported degrader dCBP-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:nude mice (female)[1]
-
Dosage:50 mg/kg
-
Administration:i.p.; single dose
-
Result:Significantly reduced p300 protein levels (relative to β-actin) in SK-HEP-1 xenograft tumor tissue compared to vehicle controls.
Significantly reduced CBP protein levels (relative to β-actin) in the tumor tissue compared to vehicle controls.
Chemical Information
-
CAS No. 3032646-96-8
-
Appearance Solid
-
Masse moléculaire 816.85
-
Formule C44H42F2N8O6
-
Color Light yellow to yellow
-
SMILES
O=C1N(C2C(NC(CC2)=O)=O)C(C(C1=C3)=CC=C3N(C4)CC4N5CCC(N6C7=CC=C(C8=C(C)ON=C8C)C=C7N=C6[C@H]9N(C%10=CC(F)=C(F)C=C%10)C(CCC9)=O)CC5)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (122.42 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: ≥ 5 mg/mL (6.12 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Fiche technique (279 KB)
-
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)
-
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 | 1.2242 mL | 6.1211 mL | 12.2422 mL | 30.6054 mL |
| 5 mM | 0.2448 mL | 1.2242 mL | 2.4484 mL | 6.1211 mL | |
| 10 mM | 0.1224 mL | 0.6121 mL | 1.2242 mL | 3.0605 mL | |
| 15 mM | 0.0816 mL | 0.4081 mL | 0.8161 mL | 2.0404 mL | |
| 20 mM | 0.0612 mL | 0.3061 mL | 0.6121 mL | 1.5303 mL | |
| 25 mM | 0.0490 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
| 30 mM | 0.0408 mL | 0.2040 mL | 0.4081 mL | 1.0202 mL | |
| 40 mM | 0.0306 mL | 0.1530 mL | 0.3061 mL | 0.7651 mL | |
| 50 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6121 mL | |
| 60 mM | 0.0204 mL | 0.1020 mL | 0.2040 mL | 0.5101 mL | |
| 80 mM | 0.0153 mL | 0.0765 mL | 0.1530 mL | 0.3826 mL | |
| 100 mM | 0.0122 mL | 0.0612 mL | 0.1224 mL | 0.3061 mL |
QC-182 Related Classifications
HY-162259 Related Classifications
Powered by Bioz