PHGDH-IN-3

CAS号

2893778-31-7

分子式

C24H18FN3O4S2

主要靶点

Dehydrogenase

仅限科研使用

Cat No : CM11658

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Synonyms

PHGDH



产品信息

CAS号 2893778-31-7
分子式 C24H18FN3O4S2
主要靶点 Dehydrogenase
主要通路 代谢
分子量 495.55
纯度 98.99%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 store at low temperature | Shipping with blue ice.
别名 PHGDH

靶点活性

PHGDH:2.8 μM|PHGDH:2.33 μM

体内活性

PHGDH-IN-3(1, 3 mg/kg;口服、静脉注射;)展现了优秀的体内药代动力学特性。[1] PHGDH-IN-3(12.5, 25, 50 mg/kg;腹腔注射;每天一次,连续31天)在PC9异种移植小鼠模型中显示出显著的抗肿瘤效果。[1]

体外活性

PHGDH-IN-3具有良好的酶抑制活性,其IC50值为2.8 μM。[1] 该化合物与PHGDH蛋白具有高结合亲和力,Kd值为2.33 μM。[1] 对于PHGDH基因扩增或过表达的细胞系,PHGDH-IN-3表现出敏感性。[1] 此外,PHGDH-IN-3能够限制在MDA-MB-468细胞中从葡萄糖到丝氨酸的新生合成。[1]

溶解度

DMSO:90.0 mg/mL (181.6 mM)

参考文献

1.Gao D, et al. Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy. J Med Chem. 2023;66(1):285-305.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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=
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C1   V1   C2   V2