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執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: K-858 is a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Long-term continuous treatment of cancer cells with K858 resulted in antiproliferative effects through the induction of mitotic cell death, and polyploidization followed by senescence. K858 exhibited potent antitumor activity in xenograft models of cancer, and induced the accumulation of mitotic cells with monopolar spindles in tumor tissues.
Name: K-858
CAS#: 72926-24-0
Chemical Formula: C13H15N3O2S
Exact Mass: 277.0885
Molecular Weight: 277.342
Elemental Analysis: C, 56.30; H, 5.45; N, 15.15; O, 11.54; S, 11.56
Synonym: K-858; K 858; K858.
IUPAC/Chemical Name: N-(4-acetyl-5-methyl-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)acetamide
InChi Key: JEFVYQYZCAVNTP-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: CC(NC1=NN(C(C)=O)C(C2=CC=CC=C2)(C)S1)=O
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
REFERENCES
1: Indorato RL, DeBonis S, Kozielski F, Garcia-Saez I, Skoufias DA.
STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting
agents according to their mode of action and target specificity. Biochem
Pharmacol. 2013 Nov 15;86(10):1441-51. doi: 10.1016/j.bcp.2013.09.003. Epub 2013
Sep 13. PubMed PMID: 24041742.
2: Nakai R, Iida S, Takahashi T, Tsujita T, Okamoto S, Takada C, Akasaka K,
Ichikawa S, Ishida H, Kusaka H, Akinaga S, Murakata C, Honda S, Nitta M, Saya H,
Yamashita Y. K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent,
induces cell death in cancer cells. Cancer Res. 2009 May 1;69(9):3901-9. doi:
10.1158/0008-5472.CAN-08-4373. Epub 2009 Apr 7. PubMed PMID: 19351824.
