| Identification | Back Directory | [Name]
CPI-203 | [CAS]
1446144-04-2 | [Synonyms]
CPI203 (CPI-203)
CPI-203 USP/EP/BP
CPI203(TEN010,JQ2,RG-6146)
CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146)
(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
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)-
(S)-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
(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 | [Molecular Formula]
C19H18ClN5OS | [MDL Number]
MFCD27997886 | [MOL File]
1446144-04-2.mol | [Molecular Weight]
399.897 |
| Chemical Properties | Back Directory | [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 | [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 | [InChIKey]
QECMENZMDBOLDR-AWEZNQCLSA-N | [SMILES]
CC1=NN=C2[C@H](CC(N)=O)N=C(C3=CC=C(Cl)C=C3)C4=C(SC(C)=C4C)N21 |
| Hazard Information | Back Directory | [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]. | [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[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. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|