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SML1212

Sigma-Aldrich

CPI203

≥98% (HPLC)

Synonym(s):

(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

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About This Item

Empirical Formula (Hill Notation):
C19H18ClN5OS
CAS Number:
1446144-04-2
Molecular Weight:
399.90
MDL number:
MFCD27997886
UNSPSC Code:
12352200
PubChem Substance ID:
329825722
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

CC1=NN=C2[C@H](CC(N)=O)N=C(C3=CC=C(Cl)C=C3)C4=C(SC(C)=C4C)N21

InChI

1S/C19H18ClN5OS/c1-9-10(2)27-19-16(9)17(12-4-6-13(20)7-5-12)22-14(8-15(21)26)18-24-23-11(3)25(18)19/h4-7,14H,8H2,1-3H3,(H2,21,26)/t14-/m0/s1

InChI key

QECMENZMDBOLDR-AWEZNQCLSA-N

Biochem/physiol Actions

CPI203 is an analog of the BET inhibitor (BETi) (+)-JQ1 and is bioavailable via oral or intraperitoneal administration. It plays an important role in lenalidomide and dexamethasone functions in in vitro and in vivo models of multiple myeloma. CPI203 inhibits proliferation, apoptosis and cell cycle arrest in A431 cell line and primary skin squamous cell carcinoma (SCC) cells.
CPI203 is an inhibitor of BRD4, a bromodomain-containing protein that binds to histones to regulate recruitment of transcription factors. BRD4 is also an RNA Pol II kinase. CPI203 blocks BRD4 kinase activity in cells and in vivo. It has shown synergistic antitumor activity with lenalidomide in bortezomib-resistant mantle cell lymphoma.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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The BET bromodomain inhibitor CPI203 improves lenalidomide and dexamethasone activity in in vitro and in vivo models of multiple myeloma by blockade of Ikaros and MYC signaling.
Diaz T, et al.
Haematologica, 102(10), 1776?1784-1776?1784 (2017)
Bromodomain protein BRD4 promotes cell proliferation in skin squamous cell carcinoma.
Xiang T, et al.
Cellular Signalling, 42, 106-113 (2018)
Yutuan Wu et al.
Journal of cancer research and clinical oncology, 148(4), 803-821 (2022-01-31)
Tumor-associated macrophages (TAMs) are known to contribute to adaptive resistance to anti-vascular endothelial growth factor (VEGF) antibody (AVA) therapy in ovarian cancer. BET (bromodomain and extra-terminal domain) inhibitors (BETi) may have unique roles in targeting TAMs. Our objective was to
Masao Nakagawa et al.
Cancer cell, 34(2), 286-297 (2018-07-31)
Adult T cell leukemia/lymphoma (ATLL) is a frequently incurable disease associated with the human lymphotropic virus type I (HTLV-I). RNAi screening of ATLL lines revealed that their proliferation depends on BATF3 and IRF4, which cooperatively drive ATLL-specific gene expression. HBZ, the
Alejandro Villar-Prados et al.
Molecular cancer therapeutics, 18(2), 421-436 (2018-11-14)
Systematic approaches for accurate repurposing of targeted therapies are needed. We developed and aimed to biologically validate our therapy predicting tool (TPT) for the repurposing of targeted therapies for specific tumor types by testing the role of Bromodomain and Extra-Terminal

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