CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146)

Alias: RO-6870810;CPI203; CPI-203; CPI 203;RO 6870810; TEN010;RG 6146; RG-6146;TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RO6870810;
Cat No.:V0424 Purity: ≥98%
CPI-203 (RO6870810, JQ-2,TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity.
CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146) Chemical Structure CAS No.: 1446144-04-2
Product category: Epigenetic Reader Domain
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146):

  • (Rac)-CPI-203
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

CPI-203 (RO6870810, JQ-2, TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity. It inhibits BRD4 with an IC50 of 37 nM in a BRD4 α-screen assay. CPI 203 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. CPI203 can enhance the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 can downregulate Myc expression, causes G1 cell cycle arrest and attenuate cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM).

Biological Activity I Assay Protocols (From Reference)
ln Vitro
CPI-203 inhibits BRD4 in vitro and in cells, but does not influence BRD4 kinase activity in vitro [1]. CPI -203 had cytostatic effects in all 9 MCL cell lines with GI50 ranging from 0.06 to 0.71 μM and had little cytotoxicity against normal PBMC from healthy volunteers. In addition, CPI -203 can effectively initiate the cell death pathway in MCL cells [2].
ln Vivo
Lenalidomide and CPI-203 (2.5 mg/kg, i.p.) together improved the anticancer effects of each individual drug by causing apoptosis in nREC-1 tumor-bearing mice and mutating MYC and IRF4 expression. [2].
Animal Protocol
2.5 mg/kg i.p.
Treatment with JQ1 derivative CPI203 inhibits BRD4 phosphorylation of CTD Ser2 in vivo. HeLa cells were transfected as above and treated with increasing concentrations of CPI203.
References
[1]. Devaiah BN, et al. 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.
[2]. Moros A, et al. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia. 2014 Oct;28(10):2049-59
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H18CLN5OS
Molecular Weight
399.90
CAS #
1446144-04-2
SMILES
ClC1C([H])=C([H])C(=C([H])C=1[H])C1C2C(C([H])([H])[H])=C(C([H])([H])[H])SC=2N2C(C([H])([H])[H])=NN=C2[C@]([H])(C([H])([H])C(N([H])[H])=O)N=1
Synonyms
RO-6870810;CPI203; CPI-203; CPI 203;RO 6870810; TEN010;RG 6146; RG-6146;TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RO6870810;
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 Data
Solubility (In Vitro)
DMSO: 79 mg/mL (197.54mM)
Water:<1 mg/mL
Ethanol: 5 mg/mL (12.5 mM)
Solubility (In Vivo)
O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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