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CPI203

Chemical Structure : CPI203

CAS No.: 1446144-04-2

CPI203 (TEN 010;JQ-2;RG-6146;RO6870810)

Catalog No.: PC-62511Not For Human Use, Lab Use Only.

CPI 203 (TEN 010, JQ-2, RG-6146, RO6870810) is a primary amide analog of (+)-JQ1and a BET bromodomain inhibitor that shows cytotoxicity against MCL cell lines with GI50 of 0.1-0.3 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CPI 203 (TEN 010, JQ-2, RG-6146, RO6870810) is a primary amide analog of (+)-JQ1and a BET bromodomain inhibitor that shows cytotoxicity against MCL cell lines with GI50 of 0.1-0.3 uM.
CPI 203 synergizes the antitumor activity of lenalidomide in bortezomib-resistant mantle cell lymphoma.
CPI 203 also enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors, overcomes resistance to ABT-199 (Venetoclax) by downregulation of BFL-1/A1 in in vitro and in vivo models of MYC+/BCL2+ double hit lymphoma.

Physicochemical Properties

M.Wt 399.897
Formula C19H18ClN5OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Moros A, et al. Leukemia. 2014 Oct;28(10):2049-59.

2. Wong C, et al. Cell Death Dis. 2014 Oct 9;5:e1450.

3. Siegel MB, et al. Oncotarget. 2015 Aug 7;6(22):18921-32.

4. Esteve-Arenys A, et al. Oncogene. 2018 Jan 22. doi: 10.1038/s41388-017-0111-1.

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