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詳細(xì)介紹 "PFI-1
產(chǎn)品活性:PFI-1 是一種有效的 BET 抑制劑,能夠有效抑制 BRD4,IC50 值為 0.22 μM。
研究領(lǐng)域:Epigenetics
作用靶點(diǎn):Epigenetic Reader Domain
In Vitro: PFI-1 has antiproliferative effects on leukemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell-cycle arrest, downregulation of MYC expression, as well as induction of apoptosis and induces differentiation of primary leukemic blasts. Cells exposed to PFI-1 show significant downregulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10, providing an alternative strategy for the specific inhibition of this well-established oncology target. PFI-1 binds to with cyclic AMP response binding protein with Kd of 49 μM. PFI-1 has an EC50 of 1.89 μM for the inhibition of IL6 production from human blood mononuclear cells stimulated by LPS. PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. PFI-1 inhibits the proliferating of three NET cell lines (Bon-1 derived from a pancreatic NET, and H727 and H720 derived from lung NETs).
In Vivo: PFI-1 administrated (1 mg/kg, i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18 mL/min/kg and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg, s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours.
相關(guān)產(chǎn)品:Anti-Cancer Compound Library | Epigenetics Compound Library | Bioactive Compound Library Plus | Histone Modification Research Compound Library | (+)-JQ-1 | A-485 | Birabresib | Curcumin | ARV-825 | ARV-771 | Molibresib | BI 2536 | C646 | 666-15 | I-BET151 | dBET1 | CPI-637 | dBET6 | Mivebresib | UNC1999 | MZ 1 | I-BRD9 | IACS-9571 Hydrochloride | SGC-CBP30 | ABBV-744 | CPI-203 | KG-501 | GNE-272 | PLX51107 | PFI-3 | Anacardic Acid | BI-7273
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