产品
编 号：F741575
分子式：C48H52F4N6O9
分子量：932.95
分子式：C48H52F4N6O9
分子量：932.95
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2417097-18-6
产品详情
生物活性：
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
体内研究：
JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts.Animal Model:NSG mice with Kelly NB cell xenografts
Dosage:40 mg/kg
Administration:Intraperitoneal injection; daily, for 21 days
Result:Suppressed tumor growth and prolonged survival.
Animal Model:CD1 mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection (Pharmacokinetic Analysis)
Result:Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.
体外研究：
JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, and induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells.JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly and NGP cells.JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis.JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, and PUMA together with the proapoptotic mediator BAX and its inhibitors BCL2 and MCL1.JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression.JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin.JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines.JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours.
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
体内研究：
JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts.Animal Model:NSG mice with Kelly NB cell xenografts
Dosage:40 mg/kg
Administration:Intraperitoneal injection; daily, for 21 days
Result:Suppressed tumor growth and prolonged survival.
Animal Model:CD1 mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection (Pharmacokinetic Analysis)
Result:Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.
体外研究：
JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, and induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells.JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly and NGP cells.JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis.JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, and PUMA together with the proapoptotic mediator BAX and its inhibitors BCL2 and MCL1.JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression.JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin.JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines.JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours.
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