[CAS NO. 592474-91-4] PKUMDL-WQ-2201

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PRODUCTS SPECIFICATIONS [592474-91-4]

Catalog

HY-123418

Brand

MCE

CAS

592474-91-4

DESCRIPTION [592474-91-4]

Overview

MDL	-
Molecular Weight	351.81
Molecular Formula	C15H14ClN3O3S
SMILES	O=C(C1=CC=C(C=C1Cl)C2=CC=C(O2)/C=N/NC(NCC)=S)O

For research use only. We do not sell to patients.

Summary

PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor ( IC ₅₀ =35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC ₅₀ s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth ^[1] ^[2] .

IC50 & Target

IC50: 35.7 μM (PHGDH WT), 69 μM (PHGDH T59A), >300 μM (PHGDH T56AK57A) ^[1]

In Vitro

PKUMDL-WQ-2201 (10 nM-100 μM; 3 d) shows good selectivity for PHGDH-amplified breast cancer cell lines, inhibits cell viability with EC ₅₀ s of 7.7 μM (MDA-MB-468) and 10.8 μM (HCC70), respectively ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PKUMDL-WQ-2201 (5-20 mg/kg; i.p.; once daily for 30 d) exhibits substantial inhibitory effects on MDA-MB-468 xenografts compared with vehicle-treated mice, without affecting the tumor growth ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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Please store the product under the recommended conditions in the Certificate of Analysis.