产品
编 号：F741844
分子式：C24H18FN3O4S2
分子量：495.55
分子式：C24H18FN3O4S2
分子量：495.55
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
50mg
询价
询价
结构图
CAS No: 2893778-31-7
产品详情
生物活性：
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.
体内研究：
PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) 表现出优异的体内药代动力学特性。PHGDH-IN-3（i.p.；12.5、25、50 mg/kg；每天一次，连续 31 天）在 PC9 异种移植小鼠模型中发挥明显的抗肿瘤作用。Animal Model:ICR mice
Dosage:1, 3 mg/kg
Administration:Oral (p.o.) and intravenous (i.v.) administration
Result: PK parameters i.v. (1 mg/kg) p.o. (3 mg/kg)
AUC (h?ng/mL)38,358 ± 14,76894,386 ± 23,416
T1/2(h)4.94 ± 0.384.74 ± 0.30
Tmax (h) 3.33 ± 1.15
CL_obs(mL/min/kg)0.48 ± 0.23
Cmax(ng/mL) 8842 ± 1755
F (%) 82.0
Animal Model:Balb/c nude mice
Dosage:12.5, 25, 50 mg/kg
Administration:Intraperitoneal (i.p.); once daily for consecutive 31 days
Result:Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth.Significantly abated the tumor weights of mice at 25 mg/ kg.
体外研究：
PHGDH-IN-3 (compound D8) 具有良好的酶促抑制活性，IC50 值为 2.8 μM。PHGDH-IN-3 对 PHGDH 蛋白具有高结合亲和力，Kd 值为2.33 μM。PHGDH-IN-3 对 PHGDH 基因扩增或过表达的细胞株具有敏感性。PHGDH-IN-3 可以限制 MDA-MB-468 细胞内葡萄糖从头合成丝氨酸。
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.
体内研究：
PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) 表现出优异的体内药代动力学特性。PHGDH-IN-3（i.p.；12.5、25、50 mg/kg；每天一次，连续 31 天）在 PC9 异种移植小鼠模型中发挥明显的抗肿瘤作用。Animal Model:ICR mice
Dosage:1, 3 mg/kg
Administration:Oral (p.o.) and intravenous (i.v.) administration
Result: PK parameters i.v. (1 mg/kg) p.o. (3 mg/kg)
AUC (h?ng/mL)38,358 ± 14,76894,386 ± 23,416
T1/2(h)4.94 ± 0.384.74 ± 0.30
Tmax (h) 3.33 ± 1.15
CL_obs(mL/min/kg)0.48 ± 0.23
Cmax(ng/mL) 8842 ± 1755
F (%) 82.0
Animal Model:Balb/c nude mice
Dosage:12.5, 25, 50 mg/kg
Administration:Intraperitoneal (i.p.); once daily for consecutive 31 days
Result:Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth.Significantly abated the tumor weights of mice at 25 mg/ kg.
体外研究：
PHGDH-IN-3 (compound D8) 具有良好的酶促抑制活性，IC50 值为 2.8 μM。PHGDH-IN-3 对 PHGDH 蛋白具有高结合亲和力，Kd 值为2.33 μM。PHGDH-IN-3 对 PHGDH 基因扩增或过表达的细胞株具有敏感性。PHGDH-IN-3 可以限制 MDA-MB-468 细胞内葡萄糖从头合成丝氨酸。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备