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PROTAK™ CPI-203
$290/ 5mg
QuantityTotal: $290
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Product Information
CAS No.1446144-04-2
NameS)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide
Purity>98.00%
FormulaC19H18ClN5OS
M.W.399.9
Solubility≥40mg/mL in DMSO
Storage/StabilityStore at -20°C
BackgroundCPI-203 is a potent, selectivie and competitive small molecule inhibitor of BET bromodomain with a mean GI50 value of 0.23μM in MCL cell lines [1].
As an inhibitor of BET proteins, CPI-203 inhibits BRD4 in vitro and in cells. It inhibits the specific Ser2 phosphorylation of both endogenous BRD4 and exogenous mutant BRD4 (BRD4 FEE-AAA) in vivo, thus blocking the recruitment of BRD4 to chromatin. CPI-203 is shown to suppress cell growth of 9 MCL cell lines. And in REC-1 cells, treatment of CPI-203 causes the effects of IRF4 expression. CPI-203 marginally activates the apoptotic program in these cells. The CPI-203-lenalidomide combination is reported to be a promising strategy in MCL cases refractory to proteasome inhibition [1, 2].
As an inhibitor of BET proteins, CPI-203 inhibits BRD4 in vitro and in cells. It inhibits the specific Ser2 phosphorylation of both endogenous BRD4 and exogenous mutant BRD4 (BRD4 FEE-AAA) in vivo, thus blocking the recruitment of BRD4 to chromatin. CPI-203 is shown to suppress cell growth of 9 MCL cell lines. And in REC-1 cells, treatment of CPI-203 causes the effects of IRF4 expression. CPI-203 marginally activates the apoptotic program in these cells. The CPI-203-lenalidomide combination is reported to be a promising strategy in MCL cases refractory to proteasome inhibition [1, 2].
Price290$
![E31P14699-1, E31P14699-2 PROTAK™ CPI-203 5mg 1446144-04-2 S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-](/img/pdfimg/E31P14699/E31P14699-002.jpg)
E31P14699-1, E31P14699-2 PROTAK™ CPI-203 5mg 1446144-04-2 S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-
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