产品
编 号：F755440
分子式：C29H30ClN5O5
分子量：564.03
分子式：C29H30ClN5O5
分子量：564.03
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2756851-99-5
产品详情
生物活性：
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
体内研究：
BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models.BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models.Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1.Parameteriv (1 mg/kg)po (10 mg/kg)
T1/2 (h)4.21±0.575.14±0.71
Cmax (ng/mL)237±11206±6
AUC0-t (ng·h/mL)579±492079±130
AUC0-∞ (ng·h/mL)588±362090±146
VZ (L/kg)21.1±2.6
CL ((mL/min)/kg)57.4±1.3
F (%)32.5
Animal Model:Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells
Dosage:25 and 50 mg/kg
Administration:Intragastric administration; daily for 19 days
Result:Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.
体外研究：
BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively. BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells.BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3.BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB.
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
体内研究：
BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models.BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models.Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1.Parameteriv (1 mg/kg)po (10 mg/kg)
T1/2 (h)4.21±0.575.14±0.71
Cmax (ng/mL)237±11206±6
AUC0-t (ng·h/mL)579±492079±130
AUC0-∞ (ng·h/mL)588±362090±146
VZ (L/kg)21.1±2.6
CL ((mL/min)/kg)57.4±1.3
F (%)32.5
Animal Model:Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells
Dosage:25 and 50 mg/kg
Administration:Intragastric administration; daily for 19 days
Result:Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.
体外研究：
BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively. BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells.BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3.BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB.
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