PKUMDL-WQ-2201
CAS No. : 592474-91-4
| Size | Price | Stock |
|---|---|---|
| 5mg | $80 | In-stock |
| 10mg | $140 | In-stock |
| 25mg | $300 | In-stock |
| 50mg | $510 | In-stock |
| 100mg | $860 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-123418 |
| M.Wt: | 351.81 |
| Formula: | C15H14ClN3O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s 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 EC50s of 7.7 μM (MDA-MB-468) and 10.8 μM (HCC70), respectively[1].
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].
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