2893778-31-7
2893778-31-7 structure
- Name: PHGDH-IN-3
- Chemical Name: PHGDH-IN-3
- CAS Number: 2893778-31-7
- Molecular Formula: C24H18FN3O4S2
- Molecular Weight: 495.55
- Catalog: Research Areas Cancer
- Create Date: 2023-04-05 11:03:45
- Modify Date: 2024-04-12 17:57:22
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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[1].
| Name | PHGDH-IN-3 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
IC50: 2.8 μM (PHGDH)[1]. Kd: 2.33 μM (PHGDH)[1] |
| 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]。 |
| 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 (h•ng/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 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. |
| References |
| Molecular Formula | C24H18FN3O4S2 |
|---|---|
| Molecular Weight | 495.55 |