BRD4/CK2-IN-1 |
Catalog No.GC66441
One-Click Copy Product Info
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BRD4/CK2-IN-1 est le premier inhibiteur actif À double cible hautement efficace et oral de BRD4/CK2 (protéine 4/caséine kinase 2 contenant du bromodomaine), avec des IC50 de 180 nM et 230 nM pour BRD4 et CK2, respectivement. BRD4/CK2-IN-1 a une forte activité anticancéreuse sans toxicités évidentes. BRD4/CK2-IN-1 induit l'apoptose et la mort cellulaire associée À l'autophagie dans le cancer du sein triple négatif (TNBC)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2756851-99-5
Sample solution is provided at 25 µL, 10mM.
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BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1]
BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB[1].
Cell Viability Assay[1]
| Cell Line: | MDA-MB-231, MDA-MB-468 cells |
| Concentration: | 0, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25 μM |
| Incubation Time: | 24 hours |
| Result: | Showed anti-proliferative rates in MDA-MB-231 and MDA-MB-468 cells (IC50 = 2.66 and 3.52 μM, respectively). |
Apoptosis Analysis[1]
| Cell Line: | MDA-MB-231, MDA-MB-468 cells |
| Concentration: | 0, 2.5, 5, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependently induced apoptosis of MDA-MB-231 and MDA-MB-468 cells. |
Western Blot Analysis[1]
| Cell Line: | MDA-MB-231, MDA-MB-468 cells |
| Concentration: | 0, 2.5, 5, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependently downregulated Bcl-2 but upregulated Bax and cleaved caspase-3. |
| Cell Line: | |
| Concentration: | |
| Incubation Time: | |
| Result: |
BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models[1].
BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models[1].
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1[1].
| Parameter | iv (1 mg/kg) | po (10 mg/kg) |
| T1/2 (h) | 4.21±0.57 | 5.14±0.71 |
| Cmax (ng/mL) | 237±11 | 206±6 |
| AUC0-t (ng.h/mL) | 579±49 | 2079±130 |
| AUC0-∞ (ng.h/mL) | 588±36 | 2090±146 |
| VZ (L/kg) | 21.1±2.6 | |
| CL ((mL/min)/kg) | 57.4±1.3 | |
| F (%) | 32.5 |
| Animal Model: | Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells[1] |
| Dosage: | 25 and 50 mg/kg |
| Administration: | Intragastric administration; daily for 19 days |
| Result: | Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg. |
| Cas No. | 2756851-99-5 | SDF | |
| Formula | C29H30ClN5O5 | M.Wt | 564.03 |
| Solubility | DMSO : 20 mg/mL (35.46 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.773 mL | 8.8648 mL | 17.7296 mL |
| 5 mM | 354.6 μL | 1.773 mL | 3.5459 mL |
| 10 mM | 177.3 μL | 886.5 μL | 1.773 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)