[CAS NO. 2893778-31-7] PHGDH-IN-3
PRODUCTS SPECIFICATIONS [2893778-31-7]
DESCRIPTION [2893778-31-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 495.55 |
| Molecular Formula | C24H18FN3O4S2 |
| SMILES | CC(C1=CC=CC(NS(=O)(C2=CC=C(C=C2)C(NC3=NC(C4=CC=CC(F)=C4)=CS3)=O)=O)=C1)=O |
Summary
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC 50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer [1] .
In Vitro
PHGDH-IN-3 (compound D8) has good enzymatic inhibitory activity with an IC
50
value of 2.8 μM
[1]
.
PHGDH-IN-3 has high binding affinity for the PHGDH protein with a K
d
value of 2.33 μM
[1]
.
PHGDH-IN-3 has sensitivity to the cell lines with the PHGDH gene amplification or overexpression
[1]
.
PHGDH-IN-3 can restrict the de novo serine synthesis from glucose within MDA-MB-468 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) exhibits excellent in vivo pharmacokinetic properties
[1]
.
PHGDH-IN-3 (i.p.; 12.5, 25, 50 mg/kg; once daily for consecutive 31 days) exertes evident antitumor efficacy in the PC9 xenograft mouse model
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | ICR mice [1] | |||||||||||||||||||||
| Dosage: | 1, 3 mg/kg | |||||||||||||||||||||
| Administration: | Oral (p.o.) and intravenous (i.v.) administration | |||||||||||||||||||||
| Result: |
|
| 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. |
Shipping
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.