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CPI-203

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CPI-203 Basic information

Product Name:
CPI-203
Synonyms:
  • (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 CPI 203
  • CPI 203 (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
  • (S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-
  • (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
  • (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic amide
  • CPI203(TEN010,JQ2,RG-6146)
  • 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-2,3,9-trimethyl-, (6S)-
  • CPI203 (CPI-203)
CAS:
1446144-04-2
MF:
C19H18ClN5OS
MW:
399.9
Product Categories:
  • Inhibitors
Mol File:
1446144-04-2.mol
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CPI-203 Chemical Properties

Boiling point:
690.4±65.0 °C(Predicted)
Density 
1.51±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
≥40 mg/mL in DMSO; insoluble in H2O; ≥6.1 mg/mL in EtOH with ultrasonic
form 
powder
pka
16.00±0.40(Predicted)
color 
white to beige
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CPI-203 Usage And Synthesis

Description

CPI-203 is a primary amide analog of (+)-JQ1, which has shown superior bioavailability with oral or i.p. administration. CPI-203 downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. CPI-203 also arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM).

Uses

CPI-203 is a bromodomain and extraterminal domain (BET) inhibitor.

Biological Activity

cpi-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].

storage

Store at -20°C

References

[1] moros a, rodríguez v, saborit-villarroya i, montraveta a, balsas p, sandy p, martínez a, wiestner a, normant e, campo e, pérez-galán p, colomer d, roué g. synergistic antitumor activity of lenalidomide with the bet bromodomain inhibitor cpi203 in bortezomib-resistant mantle cell lymphoma. leukemia. 2014 mar 18.
[2] devaiah bn, lewis ba, cherman n, hewitt mc, albrecht bk, robey pg, ozato k, sims rj 3rd, singer ds. 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.

CPI-203Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
Shanghai CanSpecsci Instrument Co., Ltd.
Tel
400-6087598 15021221957
Email
order@canspecsci.com
Mashilabs (Shanghai) Co.,Ltd.
Tel
19916721580
Email
mafarm@126.com
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CPI-203(1446144-04-2)Related Product Information