CPI-203 |
| Catalog No.GC14699 |
BET bromodomain inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1446144-04-2
Sample solution is provided at 25 µL, 10mM.
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CPI-203 is a potent, selectivie and competitive small molecule inhibitor of BET bromodomain with a mean GI50 value of 0.23μM in MCL cell lines [1].
As an inhibitor of BET proteins, CPI-203 inhibits BRD4 in vitro and in cells. It inhibits the specific Ser2 phosphorylation of both endogenous BRD4 and exogenous mutant BRD4 (BRD4 FEE-AAA) in vivo, thus blocking the recruitment of BRD4 to chromatin. CPI-203 is shown to suppress cell growth of 9 MCL cell lines. And in REC-1 cells, treatment of CPI-203 causes the effects of IRF4 expression. CPI-203 marginally activates the apoptotic program in these cells. The CPI-203-lenalidomide combination is reported to be a promising strategy in MCL cases refractory to proteasome inhibition [1, 2].
References:
[1] Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E, Pérez-Galán P, Colomer D, Roué G. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia. 2014 Mar 18.
[2] Devaiah BN, Lewis BA, Cherman N, Hewitt MC, Albrecht BK, Robey PG, Ozato K, Sims RJ 3rd, Singer DS. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.
| Cell experiment [1]: | |
|
Cell lines |
9 MCL cell lines and 2 PBMCs |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
72 hrs |
|
Applications |
In 9 MCL cell lines, CPI-203 exerted a cytostatic effect, with a mean GI50 value of 0.23 μM. At this concentration, the cytotoxicity of CPI-203 to PBMCs was below 25%, which demonstrated its selectivity. In 2 Bortezomib-resistant MCL cell lines with high MYC expression (REC-1 and JBR) and 2 Bortezomib-sensitive MCL cell lines with lower MYC expression (GRANTA-519 and JVM-2), CPI-203 at the dose of 5 μM effectively reduced MYC expression, without causing apoptosis. |
| Animal experiment [1]: | |
|
Animal models |
REC-1 tumor-bearing mice |
|
Dosage form |
2.5 mg/kg; i.p.; b.i.d. |
|
Applications |
In REC-1 tumor-bearing mice, CPI-203 alone or in combination with Lenalidomide reduced tumor volume by 44% and 62%, respectively. Moreover, tumor glucose uptake was reduced by 86% in the CPI-203 + Lenalidomide group. Immunohistochemical analysis of tumors collected from the CPI-203 + Lenalidomide group showed a decrease in the mitotic index, almost complete disappearance of MYC- and IRF4-positive cells, as well accumulation of cleaved caspase-3-positive cells. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E, Pérez-Galán P, Colomer D, Roué G. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia. 2014 Mar 18. | |
| Cas No. | 1446144-04-2 | SDF | |
| Chemical Name | (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide | ||
| Canonical SMILES | CC1=C(C)C(C(C2=CC=C(Cl)C=C2)=N[C@@H](CC(N)=O)C3=NN=C(C)N43)=C4S1 | ||
| Formula | C19H18ClN5OS | M.Wt | 399.9 |
| Solubility | ≥ 40mg/mL in DMSO | 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 | 2.5006 mL | 12.5031 mL | 25.0063 mL |
| 5 mM | 0.5001 mL | 2.5006 mL | 5.0013 mL |
| 10 mM | 0.2501 mL | 1.2503 mL | 2.5006 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 ddH2O, 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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