PHGDH-IN-3 是一种磷酸甘油酸脱氢酶(PHGDH)抑制剂，具有口服活性。PHGDH-IN-3 抑制 PHGDH，IC50值为 2.8 μM。PHGDH-IN-3 可用于癌症的研究。
| 生物活性 | PHGDH-IN-3 is an orally activephosphoglycerate dehydrogenase (PHGDH)inhibitor. PHGDH-IN-3 inhibits PHGDH with anIC50value of 2.8 μM. PHGDH-IN-3 can be used for the research ofcancer[1]. |
| IC50& Target | IC50: 2.8 μM (PHGDH)[1].
Kd: 2.33 μM (PHGDH)[1] |
体外研究
(In Vitro) | PHGDH-IN-3 (compound D8) 具有良好的酶促抑制活性，IC50值为 2.8 μM[1]。
PHGDH-IN-3 对 PHGDH 蛋白具有高结合亲和力，Kd值为2.33 μM[1]。
PHGDH-IN-3 对 PHGDH 基因扩增或过表达的细胞株具有敏感性[1]。
PHGDH-IN-3 可以限制 MDA-MB-468 细胞内葡萄糖从头合成丝氨酸[1]。
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体内研究
(In Vivo) | 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[1]。
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[1]。
| Animal Model: | ICR mice[1] | | 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 (hong/mL) | 38,358 ± 14,768 | 94,386 ± 23,416 | | T1/2(h) | 4.94 ± 0.38 | 4.74 ± 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 |
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| Animal Model: | Balb/c nude mice[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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