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编 号:F420763
分子式:C12H12N4O2
分子量:244.25
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755?μM, and the IC50 value of 0.7797?μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .

体内研究:
SKLB325 (10?mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice.Animal Model:Female athymic BALB/c nude mice
Dosage:10?mg/kg
Administration:I.p. injections every three days for eight doses total
Result:The average weight of intraperitoneal tumor nodules was 1.56?±?0.70, 1.04?±?0.62, and 0.14?±?0.11?g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.

体外研究:
SKLB325 suppresses ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth.SKLB325 (0.25-16?μM; for 24-72?h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4?μM, and the optimal duration of action is 72?h.SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro.
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