Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C13H15N3O2S |
| Molecular Weight | 277.342 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=O)NC1=NN(C(C)=O)C(C)(S1)C2=CC=CC=C2
InChI
InChIKey=JEFVYQYZCAVNTP-UHFFFAOYSA-N
InChI=1S/C13H15N3O2S/c1-9(17)14-12-15-16(10(2)18)13(3,19-12)11-7-5-4-6-8-11/h4-8H,1-3H3,(H,14,15,17)
K-858 is a small molecule inhibitor of Eg5 (kinesin spindle protein), a mitotic kinesin that plays an essential role in establishing mitotic spindle bipolarity. K-858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. K858 induces mitotic arrest, apoptosis, and cell growth inhibition in cancer cells. K-858 exhibited potent antitumor activity in xenograft models of cancer, and induced the accumulation of mitotic cells with monopolar spindles in tumor tissues.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. | 2009 May 1 |
|
| STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity. | 2013 Nov 15 |
|
| Synthesis and pharmacological screening of a large library of 1,3,4-thiadiazolines as innovative therapeutic tools for the treatment of prostate cancer and melanoma. | 2015 Nov 13 |
|
| The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells. | 2016 Aug |
Sample Use Guides
K858 exhibits antitumor activity and induces mitotic arrest in human xenograft tumor models: K858 at doses of 150 mg/kg administered orally twice for 5 days suppressed tumor
growth in an A2780 ovarian cancer xenograft model, In a HCT116 colon cancer xenograft model, at a dose of 100 mg/kg twice a day orally for 5 days, K858 also exhibited antitumor activity.
Route of Administration:
Oral
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72926-24-0
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2930014
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ZA4OIM722G
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admin on Sat Dec 16 08:01:57 GMT 2023 , Edited by admin on Sat Dec 16 08:01:57 GMT 2023
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ACTIVE MOIETY
