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Referencia número: HY-184416

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GDD-261

GDD-261 is an orally active potent allosteric PHGDH inhibitor with IC₅₀ of 61 nM and K_D of 1.17 μM. GDD-261 potently suppresses de novo serine biosynthesis via blocking the rate-limiting catalytic activity of PHGDH, elevates intracellular reactive oxygen species (ROS) and γ-H2AX levels, and reduces the GSH/GSSG ratio to trigger tumor cell oxidative stress and DNA damage. GDD-261 mainly applies to research on Erlotinib (HY-50896)-resistant EGFR-mutant non-small cell lung cancer.

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Fòrmula: C₂₄H₁₆ClF₃N₄O₄S₂
Peso molecular:580.99

Almacenamiento:

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

GDD-261 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

PHGDH

0.061 μM (IC₅₀)

PHGDH

1.17 μM (Kd)

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

Cellular Effect

Cell Line	Type	Value	Description	References
SW837	IC₅₀	8.54 μM	Inhibits SW837 cells growth for 72 h Inhibits SW837 cells growth for 72 h	42263187
HCT-116	IC₅₀	15.28 μM	Inhibits HCT-116 cells growth for 72 h Inhibits HCT-116 cells growth for 72 h	42263187
SW-620	IC₅₀	18.92 μM	Inhibits SW-620 cells growth for 72 h Inhibits SW-620 cells growth for 72 h	42263187
J82	IC₅₀	14.76 μM	Inhibits J82 cells growth for 72 h Inhibits J82 cells growth for 72 h	42263187
A375-SM	IC₅₀	22.9 μM	Inhibits A75 cells growth for 72 h Inhibits A75 cells growth for 72 h	42263187
Malme-3M	IC₅₀	30.45 μM	Inhibits Malme-3M cells growth for 72 h Inhibits Malme-3M cells growth for 72 h	42263187
SK-HEP1	IC₅₀	32.63 μM	Inhibits SK-HEP1 cells growth for 72 h Inhibits SK-HEP1 cells growth for 72 h	42263187

In Vitro

GDD-261 (120 min) exhibits broad inhibitory effects across PHGDH-overexpressing tumor cell lines^[1].
GDD-261 (1-10 μM; 1-6 h) results in a dose-dependent reduction in M+3 serine levels compared to the control, indicating effective suppression of de novo serine synthesis in MDA-MB-468 and PC9ER4 cells^[1].
GDD-261 (3 days) exhibits significantly higher inhibitory activity against PC9ER4 (IC₅₀=7.72 μM) compared with HCC827ER9 (IC₅₀=28.47 μM)^[1].
GDD-261 (2.5-5 μM; 3 days) alone exhibits comparable antiproliferative activity against PC9 and PC9ER4 cells^[1].
GDD-261 (5-10 μM; 6 days) exhibits synergistic activity with Erlotinib in PC9ER4 cells via PHGDH inhibition^[1].
GDD-261 (10 μM; 24 h) minimally affects EGFR phosphorylation or the downstream ERK and AKT signaling alone^[1].
GDD-261 (3-20 μM; 72 h) induces DNA damage and triggers apoptosis in Erlotinib-resistant cells in a dose-dependent manner^[1].
GDD-261 (1-10 μM; 1 h) induces oxidative stress in PC9 and PC9ER4 cells by altering GSH/GSSG levels^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

PC9 and PC9ER4 cells
Concentration:

2.5 μM, 5 μM
Incubation Time:

3 days
Result:

Displayed equivalent antiproliferative potency against PC9 and PC9ER4 cells alone.

Cell Proliferation Assay^[1]

Cell Line:

PC9ER4 cells
Concentration:

5 μM, 7.5 μM, 10 μM
Incubation Time:

6 days
Result:

Combined with Erlotinib markedly increased antiproliferative efficacy against resistant cells.
Showed synergy with Erlotinib only in PHGDH-proficient cells, and this combinatorial benefit vanished after PHGDH knockdown.

Western Blot Analysis^[1]

Cell Line:

PC9ER4 cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Had virtually no effect on the protein levels of p-EGFR, p-AKT, and p-ERK.

Western Blot Analysis^[1]

Cell Line:

PC9ER4 cells
Concentration:

3 μM, 10 μM, 20 μM
Incubation Time:

72 h
Result:

Increased γH2AX protein levels in a dose-dependent manner.
Increased cleaved caspase-3 protein levels in a dose-dependent manner.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_{INF_obs}	AUC_last	CL_{_obs}	MRT_{INF_obs}	V_{ss_obs}	T_max	C_max	F
Mice^[1]	1 mg/kg	i.v.	0.43 h	369 ng·h/mL	367 ng·h/mL	46.6 mL/min/kg	0.22 h	603 mL/kg	/	/	/
Mice^[1]	10 mg/kg	p.o.	0.66 h	611 ng·h/mL	608 μg·h/mL	/	0.61 h	/	0.25 h	1533 ng/mL	16.6 %

In Vivo

GDD-261 (25-50 mg/kg; p.o.; twice daily; for 20 days) achieves minimal tumor growth inhibition as a single agent but produces prominent antitumor synergy when combined with Erlotinib (30 mg/kg; once daily), with no obvious systemic or organ toxicity at therapeutic doses^[1].

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

Animal Model:

BALB/c-nude mice were injected 0.2 mL containing 5 × 10⁶ PC9ER4 cells^[1]
Dosage:

25 mg/kg, 50 mg/kg combined with Erlotinib at 30 mg/kg
Administration:

p.o., twice per day (Erlotinib for once daily), for 20 days
Result:

Exerted dose-dependent suppression of tumor volume and weight when combined with Erlotinib.
Exerted no significant influence on mouse body weight when combined with Erlotinib.
Caused no evident pathological lesions in major organs including the liver, spleen and kidney of treated mice.

Chemical Information

Peso molecular 580.99
Fòrmula C₂₄H₁₆ClF₃N₄O₄S₂
SMILES

FC(C(NC1=CC=C(C(Cl)=C1)NS(C2=CC=C(C=C2)C(NC3=NC(C4=CC(F)=CC=C4)=CS3)=O)(=O)=O)=O)F
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Wu X, et al. Structure-Based Design and Optimization of Novel PHGDH Inhibitors for Overcoming Erlotinib-Resistant Lung Cancer. J Med Chem. 2026 Jun 25;69(12):14390-14413. [Content Brief]

Calculators

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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.

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100 mg

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Actividad biológica
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- In Vitro
- In Vivo
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GDD-261

Ver todos los productos específicos de isoformas DNA/RNA Synthesis

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

GDD-261 Related Classifications

HY-184416 Related Classifications