1138549-36-6 Usage
General Description
A cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142 nM in HCT-116), but not Pol II-mediated c-myc transcription, by preventing TAF SL1 and rDNA association). Effectively inhibits Pol I-dependent proliferation among 39 cancer cell lines (IC50<1 μM) in vitro and suppresses A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion in vivo.
Biological Activity
cx-5461 is a potent and orally bioavailable small-molecule inhibitor of rrna synthesis that specifically inhibits rna polymerase (pol) i-driven transcription with ic50 value of 142 nm. cx-5461 exhibits antiproliferative activity against human pancreatic tumor cells mia paca-2, human melanoma cells a375 and colorectal carcinoma cells hct-116 with ec50 values of 74, 58, and 167 nmol/l, respectively. [1].cx-5461 was revealed to inhibit pol i transcription via promoting the stabilization of p53. in addition, cx-5461 has been demonstrated to induce autophagy and senescence but not apoptosis in mia paca-2 and a375 cell lines.
Biochem/physiol Actions
Cell permeable: yes
in vivo
cx-5461 has shown to suppress tumor volume in both mia paca-2 and a375 derived xenograft mice models [1].
references
[1] drygin d1, lin a, bliesath j, ho cb, o'brien se, proffitt c, omori m, haddach m, schwaebe mk, siddiqui-jain a, streiner n, quin je, sanij e, bywater mj,hannan rd, ryckman d, anderes k, rice wg. targeting rna polymerase i with an oral small molecule cx-5461 inhibits ribosomal rna synthesis and solid tumor growth. cancer res. 2011 feb 15;71(4):1418-30
Check Digit Verification of cas no
The CAS Registry Mumber 1138549-36-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,3,8,5,4 and 9 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1138549-36:
(9*1)+(8*1)+(7*3)+(6*8)+(5*5)+(4*4)+(3*9)+(2*3)+(1*6)=166
166 % 10 = 6
So 1138549-36-6 is a valid CAS Registry Number.
1138549-36-6Relevant articles and documents
CRYSTALLINE FORMS OF QUINOLINE ANALOGS AND SALTS THEREOF, COMPOSITIONS, AND THEIR METHODS FOR USE
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Paragraph 0244-0254, (2021/02/19)
The present invention includes crystalline forms of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (Compound I). Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms and the compositions thereof.
Facile and efficient generation of quinolone amides from esters using aluminum chloride
Schwaebe, Michael K.,Ryckman, David M.,Nagasawa, Johnny Y.,Pierre, Fabrice,Vialettes, Anne,Haddach, Mustapha
scheme or table, p. 1096 - 1100 (2011/03/22)
Quinolone esters are readily converted into the corresponding amides using aluminum chloride at room temperature in excellent yields and purities. The method is both general and scalable to multi-kilogram quantities.
