| Identification | Back Directory | [Name]
N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide | [CAS]
72926-24-0 | [Synonyms]
K 858
K858;K-858
K858 (Racemic)
N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide
N-(4-acetyl-5-methyl-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)a Cetamide
Acetamide, N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)- | [Molecular Formula]
C13H15N3O2S | [MDL Number]
MFCD00181155 | [MOL File]
72926-24-0.mol | [Molecular Weight]
277.34 |
| Chemical Properties | Back Directory | [Melting point ]
216-217 °C(Solv: ethanol (64-17-5)) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,Room Temperature | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [pka]
8.61±0.40(Predicted) | [color ]
white to off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
K858 (72926-24-0) is a selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner.1,2?It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K-858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells.1 | [Uses]
K 858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor. | [Definition]
ChEBI: N-(4-acetyl-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide is a member of benzenes. | [in vivo]
K858 (50, 150 mg/kg, p.o.) shows antitumor activity in an A2780 ovarian cancer xenograft model, also inhibits tumor grwoth in a HCT116 colon cancer xenograft model via 100 mg/kg twice a day orally for 5 days. K858 (100 mg/kg, p.o., qd ×5) displays no neurotoxic side effects in mice[1]. | [IC 50]
Eg5: 1.3 μM (IC50) | [storage]
Store at -20°C | [References]
1) Nakai et al. (2009), K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells; Cancer Res., 69 3901
2) Indorato et al. (2013), STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity; Biochem. Pharmacol.,?86?1441 |
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