产品
编 号：F751286
分子式：C27H30F3N5O3S2
分子量：593.68
分子式：C27H30F3N5O3S2
分子量：593.68
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CAS No: 2323623-93-2
产品详情
生物活性：
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=?0.79?μM, Kd=?0.89?μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
体内研究：
AS-99 (30?mg/kg; i.p.; q.d., treated for 14 consecutive days) reduces leukemia burden in mice.AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC?=?9701?hr* ng/mL and 10,699?hr* ng/mL, respectively), suitable half-life (~5–6?h) and Cmax?>10?μM.Animal Model:8- to 10-week old female NSG mice (bearing MV4;11 cells)
Dosage:30?mg/kg
Administration:I.p.; q.d., treated for 14 consecutive days
Result:Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
体外研究：
AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50?μM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L.AS-99 shows a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, with no or limited effects at 10?μM or higher concentrations.AS-99 (1-8 μM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells.AS-99 suppresses MLL fusion driven transcriptional programs.AS-99 results in a reduced number of H3K36me2 peaks when compared to the DMSO-treated cells.
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=?0.79?μM, Kd=?0.89?μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
体内研究：
AS-99 (30?mg/kg; i.p.; q.d., treated for 14 consecutive days) reduces leukemia burden in mice.AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC?=?9701?hr* ng/mL and 10,699?hr* ng/mL, respectively), suitable half-life (~5–6?h) and Cmax?>10?μM.Animal Model:8- to 10-week old female NSG mice (bearing MV4;11 cells)
Dosage:30?mg/kg
Administration:I.p.; q.d., treated for 14 consecutive days
Result:Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
体外研究：
AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50?μM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L.AS-99 shows a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, with no or limited effects at 10?μM or higher concentrations.AS-99 (1-8 μM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells.AS-99 suppresses MLL fusion driven transcriptional programs.AS-99 results in a reduced number of H3K36me2 peaks when compared to the DMSO-treated cells.
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