CPI-203 free base · Synonyms: CPI 203 · CPI203

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain.

For research use only. Not for human or veterinary use.

Target Epigenetic Reader Domain Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CPI-203 structure

CAS No.: 1446144-04-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 580.00	BP-02124-250mg	In stock	Get quote
500 mg	USD 900.00	BP-02124-500mg	In stock	Get quote
1 g	USD 1,560.00	BP-02124-1g	In stock	Get quote
2 g	USD 2,477.00	BP-02124-2g	In stock	Get quote

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Description

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).

Biological activity

In Vitro CPI-203 inhibits BRD4 in vitro and in cells, but does not affect BRD4 kinase activity in vitro[1]. CPI-203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, CPI-203 efficiently activates the cell death program in MCL cells. In Vivo CPI-203 (2.5 mg/kg, i.p.) combined with lenalidomide, enhances the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis in n REC-1 tumor-bearing mice.

Identifiers

SMILES: CC1=NN=C2[C@H](CC(N)=O)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1
InChIKey: QECMENZMDBOLDR-AWEZNQCLSA-N

Specifications

MW (average): 399.8970
Formula: C₁₉H₁₈ClN₅OS
CAS No.: 1446144-04-2
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 year;

Solubility

Soluble in DMSO

Documents

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.

Same target

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Same research area

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