[CAS NO. 304481-72-9] PKUMDL-WQ-2101
PRODUCTS SPECIFICATIONS [304481-72-9]
DESCRIPTION [304481-72-9]
Overview
| MDL | MFCD00589939 |
|---|---|
| Molecular Weight | 317.25 |
| Molecular Formula | C14H11N3O6 |
| SMILES | O=C(C1=CC=C(C=C1O)O)N/N=C/C2=CC([N+]([O-])=O)=CC=C2O |
Summary
PKUMDL-WQ-2101 is a non-NAD + -competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC 50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity [1] .
IC50 & Target
IC50: 34.8 μM (PHGDH) [1]
In Vitro
PKUMDL-WQ-2101 (72 hours) shows dose-dependent suppression effects on the cell viability at micromolar concentrations, with good selectivity for PHGDH amplified breast cancer cell lines. The antitumor activities of PKUMDL-WQ-2101 in the two PHGDH amplified breast cancer cell lines (MDA-MB-468 and HCC70) are 7.70 μM and 10.8 μM, respectively
[1]
.
PKUMDL-WQ-2101 (2.5-40 μM; 24 hours) causes cell cycle arrest in MDA-MB-468 cells
[1]
.
PKUMDL-WQ-2101 (37 μM; 24 hours) decreases de novo serine synthesis and metabolism downstream of the serine synthesis pathway, with effects comparable to PHGDH genetic deletion
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | MDA-MB-468 cells |
| Concentration: | 2.5 μM, 5.0 μM, 20 μM and 40 μM |
| Incubation Time: | 24 hours |
| Result: | Caused cell cycle arrest. |
In Vivo
PKUMDL-WQ-2101 (5-20 mg/kg; i.p; daily; for 30 days) exhibits substantial inhibitory effects on MDA-MB-468 xenografts [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | NOD.CB17 Scid/J mice injected with MDA-MB-468 cells [1] |
| Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg |
| Administration: | i.p; daily; for 30 days |
| Result: | Exhibited substantial inhibitory effects on MDA-MB-468 xenografts. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.