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Art. -Nr.: HY-184449

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PHGDH-IN-7

PHGDH-IN-7 is an orally active Cys281-targeted covalent noncompetitive PHGDH inhibitor with an enzymatic IC₅₀ of 0.8 μM, MST K_d of 3.4 μM, and K_i of 2.82 μM. PHGDH-IN-7 disrupts PHGDH homodimer formation. PHGDH-IN-7 blocks cellular de novo serine synthesis. PHGDH-IN-7 elevates intracellular ROS levels and inhibits DNA replication. PHGDH-IN-7 resensitizes EGFR-TKI-resistant lung adenocarcinoma cells. PHGDH-IN-7 suppresses triple-negative breast tumor growth with no obvious systemic toxicity. PHGDH-IN-7 serves as a tool compound for PHGDH-dependent tumor research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₂H₄₀N₁₀O₂
Molecular Weight:596.73

Speicherung:

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

PHGDH-IN-7 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC70	IC₅₀	4.8 μM	Inhibits the growth of HCC70 cells for 72 h. Inhibits the growth of HCC70 cells for 72 h.	42284116
MDA-MB-468	IC₅₀	1.8 μM	Inhibits the growth of MDA-MB-468 cells for 72 h. Inhibits the growth of MDA-MB-468 cells for 72 h.	42284116
ZR-75-1	IC₅₀	50.2 μM	Inhibits the growth of ZR-75-1 cells for 72 h. Inhibits the growth of ZR-75-1 cells for 72 h.	42284116
PC-9	IC₅₀	2.3 μM	Inhibits the growth of PC-9 cells for 72 h. Inhibits the growth of PC-9 cells for 72 h.	42284116
HCT-116	IC₅₀	5.3 μM	Inhibits the growth of HCT-116 cells for 72 h. Inhibits the growth of HCT-116 cells for 72 h.	42284116

In Vitro

PHGDH-IN-7 (Compound D5-2) (72 h) exhibits potent activity against PHGDH-dependent MDA-MB-468 cells with a cellular IC50 of 1.8 μM, and displays markedly weaker anti-proliferative effects in PHGDH-independent cell lines^[1].
PHGDH-IN-7 (40 μM; 3 min) effectively targets PHGDH protein in MDA-MB-468 cells^[1].
PHGDH-IN-7 (1.5-3 μM; 48 h) relies primarily on PHGDH for its antiproliferative potency in MDA-MB-468 cells^[1].
PHGDH-IN-7 (2.5-10 μM; 8 h) inhibits the serine synthesis in MDA-MB-468 cells^[1].
PHGDH-IN-7 (2.5-10 μM; 24 h) suppresses DNA synthesis and elevates intracellular ROS levels in MDA-MB-468 cells^[1].
PHGDH-IN-7 (1-5 μM; 48 h) impairs clonogenic growth of MDA-MB-468 and HCT116 cells^[1].
PHGDH-IN-7 (5-20 μM; 2 weeks) preferentially inhibits colony formation of PHGDH-high HCC827ER9 cells compared to PHGDH-low parental HCC827 and HCC827OR lines^[1].
PHGDH-IN-7 (1-2 μM; 48 h) restores Erlotinib (HY-50896) sensitivity to HCC827ER9 cells and produces synergistic antiproliferative effects^[1].
PHGDH-IN-7 (5-10 μM; 48 h) requires higher concentrations to resensitize Osimertinib (HY-15772)-resistant HCC827OR cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

40 μM
Incubation Time:

3 min
Result:

Decreased the thermal stability of PHGDH in MDA-MB-468 cells.

Cell Viability Assay^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

1.5 μM, 3 μM
Incubation Time:

48 h
Result:

Displayed markedly weakened inhibitory activity against MDA-MB-468 cells following PHGDH RNAi knockdown.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

2.5 μM, 5 μM, 10 μM
Incubation Time:

24 h
Result:

Suppressed DNA synthesis in MDA-MB-468 cells, as measured by EdU incorporation.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-468 cells, HCT116 cells
Concentration:

1 μM, 2.5 μM, 5 μM
Incubation Time:

48 h
Result:

Reduced the clonogenic capacity of MDA-MB-468 and HCT116 cells.

Cell Proliferation Assay^[1]

Cell Line:

HCC827ER9 cells, HCC827 cells, HCC827OR cells
Concentration:

5 μM, 10 μM, 20 μM
Incubation Time:

2 weeks
Result:

Exhibited potent inhibition against PHGDH-high HCC827ER9 cells.
Showed weaker activity against PHGDH-low parental HCC827 and HCC827OR cells.

Cell Proliferation Assay^[1]

Cell Line:

HCC827ER9 cells
Concentration:

1 μM, 2 μM
Incubation Time:

48 h
Result:

Significantly restored Erlotinib (HY-50896) sensitivity in HCC827ER9.

Cell Proliferation Assay^[1]

Cell Line:

HCC827OR cells
Concentration:

5 μM, 10 μM
Incubation Time:

48 h
Result:

Needed higher concentrations to resensitize HCC827OR cells to Osimertinib (HY-15772).

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	CL	V_ss	MRT_0-t	F
Mice^[1]	10 mg/kg	i.v.	50390 ng/mL	0.083 h	0.16 h	100763 ng/mL·h	1.68 mL/min/kg	24 mL/kg	0.0033 h	/
Mice^[1]	30 mg/kg	i.p.	15601 ng/mL	0.33 h	0.74 h	22697 ng/mL·h	/	/	1.14 h	7.51 %
Mice^[1]	30 mg/kg	p.o.	16929 ng/mL	0.33 h	0.20 h	8545 ng/mL·h	/	/	0.38 h	2.83 %

In Vivo

PHGDH-IN-7 (Compound D5-2) (25-50 mg/kg; i.p.; twice daily; for 21 days) produces dose-dependent antitumor activity in MDA-MB-468 xenograft NOD-SCID female mice without systemic toxicity^[1].

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

Animal Model:

Female NOD-SCID mice bearing MDA-MB-468 triple-negative breast cancer xenografts^[1]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

i.p.; twice daily; for 21 days
Result:

Did not cause noticeable loss in body weight, and no other signs of toxicity were observed at two dosages.
Significantly inhibited tumor size and weight.

Chemical Information

Molecular Weight 596.73
Formel C₃₂H₄₀N₁₀O₂
SMILES

CNC1=NC(N[C@H](C(N)=O)CC2=CC=C(C3=CC=C(N(C)C)N=C3)C=C2)=NC(N4CC[C@]5(CCN(C(C#CC)=O)C5)CC4)=N1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Feng L, et al. Discovery of a Covalent Inhibitor Targeting the PHGDH Dimer Interface with Antitumor Efficacy. J Med Chem. 2026 Jun 25;69(12):14530-14554. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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PHGDH-IN-7

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PHGDH-IN-7 Related Classifications

HY-184449 Related Classifications