产品
编 号：F565272
分子式：C59H62F2N9O12P
分子量：1158.15
分子式：C59H62F2N9O12P
分子量：1158.15
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2429877-44-9
产品详情
生物活性：
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice.?SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model.?SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model.Animal Model:SCID female mice (MOLM-16 xenograft model)
Dosage:25, 50, 100 mg/kg
Administration:i.v.; weekly dosing for 4 weeks
Result:At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.
体外研究：
SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis. SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC50＜2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines.SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells.
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice.?SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model.?SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model.Animal Model:SCID female mice (MOLM-16 xenograft model)
Dosage:25, 50, 100 mg/kg
Administration:i.v.; weekly dosing for 4 weeks
Result:At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.
体外研究：
SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis. SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC50＜2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines.SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells.
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