934541-31-8 Usage
Uses
Different sources of media describe the Uses of 934541-31-8 differently. You can refer to the following data:
1. A novel Aurora B kinase inhibitor with potential antineoplastic activity. It binds to and inhibits the activity of Aurora B, which may result in a decrease in the proliferation of tumor cells that overexpress Aurora B. Aurora B is a positive regulator of mitosis that functions in the attachment of the mitotic spindle to the centromere; the segregation of sister chromatids to each daughter cell; and the separation of daughter cells during cytokinesis.
2. A novel Aurora B kinase inhibitor with potential antineoplastic activity. It binds to and inhibits the activity of Aurora B, which may result in a decrease in the proliferation of tumor cells that overexpress Aurora B. Aurora B is a positive regulator of mitosis that functions in the attachment of the mitotic spindle to the centromere; the segregation of sister chromatids to each daughter cell; and the separation of daughter cells during cytokinesis. It is a COVID19-related research product.
Biological Activity
protein kinases aurora a, b, and c play crucial roles during mitosis and cell division, are frequently elevated in cancer, and represent attractive targets for therapeutic intervention. tak-901 is a novel, multitargeted aurora b kinase inhibitor derived from a novel azacarboline kinase hinge-binder chemotype.
in vitro
tak-901 exhibited time-dependent, tight-binding inhibition of aurora b, but not aurora a. consistently, tak-901 suppressed cellular histone h3 phosphorylation and induced polyploidy. in various human cancer cell lines, tak-901 inhibited cell proliferation with effective concentration values from 40 to 500 nmol/l. tak-901 potently inhibited only a few kinases other than aurora b in intact cells, including flt3 and fgfr2 [1].
in vivo
in rodent xenografts, tak-901 exhibited potent activity against multiple human solid tumor types, and complete regression was found in the ovarian cancer a2780 model. in vivo biomarker studies showed that tak-901 induced pd responses consistent with aurora b inhibition and correlating with retention of tak-901 in tumor tissue. [2].
IC 50
0.0017, 0.021 for aurora-b/incenp and aurora-a/tpx2, respectively
references
[1] farrell p, shi l, matuszkiewicz j, balakrishna d, hoshino t, zhang l, elliott s, fabrey r, lee b, halkowycz p, sang b, ishino s, nomura t, teratani m, ohta y, grimshaw c, paraselli b, satou t, de jong r. biological characterization of tak-901, an investigational, novel, multitargeted aurora b kinase inhibitor. mol cancer ther. 2013;12(4):460-70.
Check Digit Verification of cas no
The CAS Registry Mumber 934541-31-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,4,5,4 and 1 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 934541-31:
(8*9)+(7*3)+(6*4)+(5*5)+(4*4)+(3*1)+(2*3)+(1*1)=168
168 % 10 = 8
So 934541-31-8 is a valid CAS Registry Number.
InChI:InChI=1S/C28H32N4O3S/c1-5-36(34,35)21-8-6-7-19(14-21)23-15-22(28(33)30-20-9-11-32(4)12-10-20)18(3)26-25(23)24-13-17(2)16-29-27(24)31-26/h6-8,13-16,20H,5,9-12H2,1-4H3,(H,29,31)(H,30,33)
934541-31-8Relevant articles and documents
KINASE INHIBITORS
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, (2009/12/02)
Compounds are provided for use with kinases that comprise a compound selected from the rou consistin of:wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods an intermediates useful for making the compounds; and methods of using said compounds.
POLYMORPHS OF HYDROCHLORIDE SALT OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PYRIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR
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Page/Page column 24-25, (2009/10/31)
Polymorphic forms of the hydrochloride salt of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound 1) which has the formula: and compositions thereof, wherein the Compoun
