1037184-44-3 Usage
Chemical Properties
A crystalline solid
Uses
Different sources of media describe the Uses of 1037184-44-3 differently. You can refer to the following data:
1. YK-4-279 is a small molecule inhibitor of EWS-FLI1 protein, and has been shown to disrupt the mitotic progression of neuroblastoma cells, and potentially other cancers.
2. An oncogenic fusion protein found in Ewing's sarcoma, a family of undifferentiated tumors which occur throughout the body. The binding of ES-FLI1 to RNA helicase A (RHA) promotes its oncogenic function. Inhibits protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing's sarcoma tumor cell lines with IC50 values ranging from 0.5 to 2 μM.1 At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing's sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
Biological Activity
yk 4-279 is an inhibitor of rna helicase a (rha) binding to the oncogenic transciption factor ews-fli1.ews-fli1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. ews-fli1 binding to rna helicase a (rha) is important for its oncogenic function.
in vitro
esft cells treated with yk-4-279 showed a dissociation of ews-fli1 from rha by 10 mm, consistent with the kd value. the ews-fli1–transfected cells showed a dose-dependent decrease in promoter activity when treated for 18 h with 3 mm and 10 mm yk-4-279. yk-4-279 was relatively specific for esft cells as compared to the nontransformed hek293 cells [1].
in vivo
the tumor growth rate of yk-4-279–treated mice bearing chp-100 was lower than that in mice having pc3 prostate tumors. the cumulative data from five independent experiments with the esft xenografts (tc71 and chp-100) show a marked overall tumor reduction in the yk-4-279–treated mice. pathological analysis of mice treated with yk-4-279 did not show any signs of toxicity, except for sterile inflammatory lesions in the abdominal cavities of mice [1].
references
[1] erkizan hv, kong y, merchant m, schlottmann s, barber-rotenberg js, yuan l, abaan od, chou th, dakshanamurthy s, brown ml, uren a, toretsky ja. a small molecule blocking oncogenic protein ews-fli1 interaction with rna helicase a inhibits growth of ewing's sarcoma. nat med. 2009;15(7):750-6.
Check Digit Verification of cas no
The CAS Registry Mumber 1037184-44-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,3,7,1,8 and 4 respectively; the second part has 2 digits, 4 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1037184-44:
(9*1)+(8*0)+(7*3)+(6*7)+(5*1)+(4*8)+(3*4)+(2*4)+(1*4)=133
133 % 10 = 3
So 1037184-44-3 is a valid CAS Registry Number.
1037184-44-3Relevant articles and documents
INDOLINE ANALOGS AND USES THEREOF
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Paragraph 0134, (2017/10/31)
Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for id
TARGETING OF EWS-FLI1 AS ANTI-TUMOR THERAPY
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Page/Page column 33; 35, (2008/12/07)
Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying
