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PHGDH-IN-3

PHGDH-IN-3 是一种具有口服活性的磷酸甘油酸脱氢酶 (PHGDH) 抑制剂， 对 PHGDH 具有抑制作用，IC50 值为 2.8 μM。PHGDH-IN-3 可用于研究癌症。

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

验证数据展示

  • CAS No.: 2893778-31-7

    PHGDH-IN-3
    CAS#: 2893778-31-7

产品信息

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.8 μM against PHGDH. PHGDH-IN-3 can be used in studies about cancer.

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
别名

靶点活性

PHGDH:2.8 μM|PHGDH:2.33 μM

体内活性

PHGDH-IN-3 (compound D8) (1, 3 mg/kg; p.o., i.v.; ) exhibits excellent in vivo pharmacokinetic properties.[1] PHGDH-IN-3 (12.5, 25, 50 mg/kg; i.p.; once daily for 31 days) exerted significant antitumor effects in a PC9 xenograft mouse model.[1]

体外活性

PHGDH-IN-3 (compound D8) has good enzymatic inhibitory activity with an IC50 value of 2.8 μM.[1] PHGDH-IN-3 has a high binding affinity for PHGDH protein with a Kd value of 2.33 μM.[1] PHGDH-IN-3 is sensitive to cell lines with amplified or overexpressed PHGDH genes.[1] PHGDH-IN-3 restricts the de novo synthesis of serine from glucose in MDA-MB-468 cells.[1]

溶解度

DMSO:90.0 mg/mL (181.6 mM),ultrasonic and warming and heat to 70°C

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)
×
=
×
C1   V1   C2   V2