PC10709
PC10709 is a p53Y220C reactivator with an EC50 value of 0.06 μM. PC10709 shows off-target binding to wild-type p53 and p53-R175H (Kd = 0.38-0.48 μM). PC10709 induces MDM2 and BBC3. PC10709 inhibits tumor growth in gastric cancer models.
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- No. CAS: 2127092-19-5
- Fòrmula: C27H31F3N4O3S
- Peso molecular:548.62
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Actividad biológica
Descripciòn
PC10709 is a p53Y220C reactivator with an EC50 value of 0.06 μM. PC10709 shows off-target binding to wild-type p53 and p53-R175H (Kd = 0.38-0.48 μM). PC10709 induces MDM2 and BBC3. PC10709 inhibits tumor growth in gastric cancer models[1][2].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NUGC-3 | IC50 |
2.8 μM
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Antiproliferative activity against human NUGC-3 gastric cancer cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human NUGC-3 gastric cancer cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| NUGC-3 | IC50 |
3.6 μM
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Antiproliferative activity against human NUGC-3-KD cells with p53-Y220C knockdown assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human NUGC-3-KD cells with p53-Y220C knockdown assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| BXPC-3 | IC50 |
2.2 μM
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Antiproliferative activity against human BxPC-3 pancreatic cancer cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human BxPC-3 pancreatic cancer cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| Huh-7 | IC50 |
2.1 μM
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Antiproliferative activity against human HuH-7 hepatocellular carcinoma cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human HuH-7 hepatocellular carcinoma cells harboring p53-Y220C assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| NUGC-4 | IC50 |
4.9 μM
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Antiproliferative activity against human NUGC-4 gastric cancer cells with wild-type p53 assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human NUGC-4 gastric cancer cells with wild-type p53 assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| HEK-293T | IC50 |
3.9 μM
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Antiproliferative activity against human HEK-293T embryonic kidney cells with wild-type p53 assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
Antiproliferative activity against human HEK-293T embryonic kidney cells with wild-type p53 assessed as viability reduction after 3-day exposure by CCK-8 assay with absorbance at 450 nm.
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42268678 |
| NUGC-3 | IC50 |
1.7 μM
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Antiproliferative activity against human NUGC-3 gastric cancer cells harboring p53-Y220C assessed as viability reduction by CCK-8 assay as reported in the Figure 1 summary.
Antiproliferative activity against human NUGC-3 gastric cancer cells harboring p53-Y220C assessed as viability reduction by CCK-8 assay as reported in the Figure 1 summary.
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42268678 |
In Vitro
Anti-cancerApoptosisOthers
Anti-cancer
PC10709 (up to 10 µM; 3 days) inhibits the proliferation of p53-Y220C mutant cell lines, with IC50 values in the low micromolar range (NUGC-3 2.8 µM; BxPC-3 2.2 µM; HuH-7 2.1 µM)[2].
Anti-cancer
Apoptosis
Others
PC10709 (10-60 min) activates DNA binding of purified recombinant p53 Y220C with an EC50 of 0.06 μM[1].
PC10709 (1-10 µM) activates p53-Y220C DNA binding in the HTRF assay, EC50 = 0.064 µM[2].
PC10709 binds p53-Y220C with high affinity by SPR (KD = 10.3 nM), but also shows measurable binding to WT p53 and p53-R175H[2].
PC10709 (10 µM) selectively thermodynamically stabilizes p53-Y220C without destabilizing WT p53 or p53-R273H[2].
PC10709 (10 µM; 6 h) enhances the binding of p53-Y220C to p53 consensus DNA in NUGC-3 cell lysates[2].
PC10709 (1-10 µM) activates p53-Y220C DNA binding in the HTRF assay, EC50 = 0.064 µM[2].
PC10709 binds p53-Y220C with high affinity by SPR (KD = 10.3 nM), but also shows measurable binding to WT p53 and p53-R175H[2].
PC10709 (10 µM) selectively thermodynamically stabilizes p53-Y220C without destabilizing WT p53 or p53-R273H[2].
PC10709 (10 µM; 6 h) enhances the binding of p53-Y220C to p53 consensus DNA in NUGC-3 cell lysates[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
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Cell Line:NUGC-3 (p53-Y220C), NUGC-3-KD, BxPC-3 (p53-Y220C), HuH-7 (p53-Y220C), NUGC-4 (WT p53), and HEK-293T (WT p53) cells
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Concentration:10 µM starting, 3-fold serial dilution
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Incubation Time:3 days
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Result:IC50 values were: NUGC-3 (Y220C) 2.8 µM; NUGC-3 (Y220C-KD) 3.6 µM; BxPC-3 (Y220C) 2.2 µM; HuH-7 (Y220C) 2.1 µM; NUGC-4 (WT p53) 4.9 µM; HEK-293T (WT p53) 3.9 µM; selectivity ratio (KD/Parent) 1.3.
Figure 1 summary lists NUGC-3 IC50 = 1.7 µM.
Real Time qPCR[2]
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Cell Line:NUGC-3 gastric cancer cells (p53-Y220C)
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Concentration:15 and 30 µM
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Incubation Time:2 h
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Result:Figure 4 bar graphs showed increased transcript levels for BAX, FAS, GADD45A, MDM2, CDKN1A, and BBC3 at 15 and 30 µM.
In Vivo
Anti-cancer
PC10709 (50 mg/kg; i.p.; once daily; up to 21 days or until ethical endpoint) inhibits NUGC-3 xenograft tumor growth by 42.8% TGI and induces MDM2 and BBC3 transcription in BALB/c nude male mice with gastric cancer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old)[2]
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Dosage:50 mg/kg
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Administration:i.p.; once daily; for up to 21 days or until ethical endpoint
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Result:At 50 mg/kg, achieved a tumor growth inhibition (TGI) rate of 42.8% in the NUGC-3 xenograft model.
At 50 mg/kg, induced pronounced upregulation of MDM2 and BBC3 mRNA in excised tumor tissues.
Chemical Information
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No. CAS 2127092-19-5
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Peso molecular 548.62
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Fòrmula C27H31F3N4O3S
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SMILES
O=S(C1=CC=C(C(OC)=C1)NCC#CC2=CC3=C(N2CC(F)(F)F)C=CC=C3NC4CCN(CC4)C)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Pureza:
99.98%
Assay:
99.98%
ee.:
99.98%
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