Art. -Nr.: HY-170952

LYG-409

Name: LYG-409
Brand: MedChemExpress
SKU: HY-170952
Price: 197.00 USD
Availability: InStock
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LYG-409 is a highly potent, selective, and orally active GSPT1 molecular glue degrader. LYG-409 induces GSPT1 degradation in KG-1 cells with a DC₅₀ of 7.87 nM. LYG-409 binds to Cereblon with an IC₅₀ of 191 nM, promotes the formation of the CRBN-GSPT1 ternary complex, and induces proteasome-dependent degradation of GSPT1. LYG-409 exhibits broad antiproliferative and GSPT1-degrading activities in a variety of hematologic and solid tumor cells. LYG-409 can be used for studies related to GSPT1-targeted protein degradation, acute myeloid leukemia, and prostate cancer.

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Reinheit: 98.11%
CAS. Nr.: 3053857-55-6
Formel: C₂₅H₂₀F₃N₃O₆
Molecular Weight:515.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LYG-409 Chemical Structure

CAS. Nr.: 3053857-55-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

eRF3a/GSPT1

7.87 nM (DC₅₀)

Alle Eukaryotic Release Factor (eRF) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC50	0.008 μM	Antiproliferative activity against human cancer MV4-11 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer MV4-11 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
OCI-AML-3	IC50	0.084 μM	Antiproliferative activity against human cancer OCI-AML3 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer OCI-AML3 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
U-937	IC50	0.029 μM	Antiproliferative activity against human cancer U937 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer U937 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
SU-DHL-4	IC50	0.34 μM	Antiproliferative activity against human cancer SU-DHL-4 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer SU-DHL-4 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
WSUDLCL2	IC50	0.017 μM	Antiproliferative activity against human cancer WSU-DLCL2 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer WSU-DLCL2 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
22Rv1	IC50	0.030 μM	Antiproliferative activity against human cancer 22Rv1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer 22Rv1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
T47D	IC50	0.047 μM	Antiproliferative activity against human cancer T47D cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer T47D cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
MDA-MB-231	IC50	0.016 μM	Antiproliferative activity against human cancer MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
MDA-MB-453	IC50	0.046 μM	Antiproliferative activity against human cancer MDA-MB-453 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer MDA-MB-453 cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
Hs-578T	IC50	0.081 μM	Antiproliferative activity against human cancer Hs578t cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human cancer Hs578t cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008
BEAS-2B	IC50	0.37 μM	Antiproliferative activity against human normal lung epithelial BEAS-2B cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human normal lung epithelial BEAS-2B cells assessed as reduction in cell proliferation incubated for 72 hrs by CCK-8 assay.	39854008

In Vitro

LYG-409 (4 h) induces time- and dose-dependent degradation of GSPT1 via the ubiquitin-proteasome pathway in KG-1 acute myeloid leukemia cells, with a DC50 of 7.87 nM^[1].
LYG-409 (200 nM; 72 h) potently inhibits the proliferation of KG-1 acute myeloid leukemia cells, with an IC₅₀ of 9.50 nM, and induces 92.39% GSPT1 degradation at a concentration of 200 nM^[1].
LYG-409 (72 h) inhibits the proliferation of various hematologic and solid tumor cells, with IC₅₀ values of 0.010, 0.008, 0.029, 0.017, 0.030, and 0.016 μM against KG-1, MV4-11, U937, WSU-DLCL2, 22Rv1, and MDA-MB-231 cells, respectively^[1].
LYG-409 (at multiple concentrations; 4-24 h) induces dose-dependent GSPT1 degradation in a variety of hematological and solid tumor cell lines, with DC₅₀ values ranging from 2.77 nM (22Rv1) to 90 nM (Molm-13)^[1].
LYG-409 (191 nM) binds to human CRBN with high affinity, with an IC₅₀ of 191 nM^[1].
LYG-409 (100 nM; 2-12 h) reduces GSPT1 protein levels in a time-dependent manner in KG-1 cells, accompanied by a decrease in C-MYC protein levels^[1].
LYG-409 (1-10 μM) does not inhibit CYP3A4 at the concentration of 10 μM, exhibits moderate hERG inhibitory activity, has acceptable permeability, and shows a high plasma protein binding rate (99.03%)^[1].
LYG-409 (24 h) induces dose-dependent degradation of GSPT1 in 22Rv1, MDA-MB-453, MDA-MB-231 and Hs578t cells, with DC₅₀ values of 2.77, 4.05, 6.73 and 7.37 nM, respectively^[1].
LYG-409 (10-200 nM; 12 h) induces concentration-dependent apoptosis in KG-1 acute myeloid leukemia cells, with 75.9% apoptotic cells observed after treatment with 200 nM for 12 h^[1].
LYG-409 induces GSPT1 degradation in a concentration-dependent manner in MV4-11 and Molm-13 cells, with DC₅₀ values of 16 nM and 90 nM at 4 h, respectively^[1].
LYG-409 (4 h) promotes the formation of the CRBN-GSPT1 ternary complex in a concentration-dependent manner in HEK293T cells expressing SmBiT-CRBN and LgBiT-GSPT1^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

human acute myeloid leukemia KG-1 cells
Concentration:

200 nM
Incubation Time:

72 h
Result:

Induced 92.39% degradation of GSPT1 protein in KG-1 cells.

Apoptosis Analysis^[1]

Cell Line:

human acute myeloid leukemia KG-1 cells
Concentration:

10 nM; 50 nM; 200 nM
Incubation Time:

12 h
Result:

Resulted in 22.4% early and late apoptotic cells at 10 nM.
Resulted in 46.8% early and late apoptotic cells at 50 nM.
Resulted in 75.9% early and late apoptotic cells at 200 nM.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_last	AUC_inf	T_1/2	MRT_{INF_obs}	F	CL	C₀	V_{ss_obs}
Rat^[1]	2 mg/kg	i.v.	/	/	/	4349 ng·h/mL	1.53 h	/	/	8.1 mL/min/kg	/	/
Rat^[1]	10 mg/kg	p.o.	3460 ng/mL	0.33 h	/	4978 ng·h/mL	3.71 h	/	22.93 %	/	/	/
Mice^[1]	2 mg/kg	i.v.	/	/	8812 ng·h/mL	8823 ng·h/mL	1.12 h	1.07 h	/	3.8 mL/min/kg	16143 ng/mL	0.24 L/kg
Mice^[1]	10 mg/kg	p.o.	2550 ng/mL	0.41 h	6147 ng·h/mL	6406 ng·h/mL	1.82 h	2.91 h	13.9 %	/	/	/
Dog^[1]	2 mg/kg	i.v.	/	/	2170 ng·h/mL	2170 ng·h/mL	1.01 h	0.59 h	/	16.9 mL/min/kg	9030 ng/mL	0.54 L/kg
Dog^[1]	10 mg/kg	p.o.	247 ng/mL	0.50 h	391 ng·h/mL	442 ng·h/mL	4.58 h	2.64 h	3.6 %	/	/	/

In Vivo

LYG-409 (15 or 30 mg/kg/day; p.o.; for 14 consecutive days) inhibits tumor growth in a female Balb/c nude mouse xenograft model of MV4-11 acute myeloid leukemia, with tumor growth inhibition (TGI) rates of 75.29% and 94.34%, respectively. No significant body weight loss or mortality is observed during the administration period^[1].
LYG-409 (60 mg/kg/day; p.o.; once daily; 18 days) achieves a TGI of 104.49% in the 22Rv1 prostate cancer xenograft model of male Balb/c nude mice. At the end of the study, 87.5% (7/8) of the mice achieve complete remission, with no significant changes observed in behavior, diet or body weight^[1].
LYG-409 (60 mg/kg; single oral gavage) reduces the GSPT1 protein level in tumor tissues by more than 70% at 6 h post-administration in 22Rv1 xenograft mice, and the GSPT1 level remains below 50% of that in the control group at 24 h^[1].

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

Animal Model:

BALB/c nude (female, 4-6 weeks old, 16-20 g, subcutaneously injected with 1 × 10⁷ MV4−11 cells)^[1]
Dosage:

5 mg/kg; 15 mg/kg; 30 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Showed no significant tumor growth inhibition at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 75.29% at 15 mg/kg.
Achieved a TGI rate of 94.34% at 30 mg/kg.
Caused no significant body weight loss, mortality, or tissue injuries in any dose group.

Animal Model:

BALB/c nude (male, 4-6 weeks old, 16-20 g, subcutaneously injected with 5 × 10⁶ 22Rv1 cells)^[1]
Dosage:

60 mg/kg (daily dosing); 60 mg/kg (single dose)
Administration:

p.o. (daily for 18 days); p.o. (single dose)
Result:

Achieved a TGI rate of 104.49% with 87.5% of mice showing complete tumor response at 60 mg/kg daily.
Reduced GSPT1 protein levels by >70% at 6 h post-administration, and levels remained below 50% of control at 24 h after a single 60 mg/kg dose.
Caused no significant body weight loss or changes in behavior/diet during 18 days of administration.

Animal Model:

Sprague-Dawley (SD) (male and female, weight matching across groups)^[1]
Dosage:

100 mg/kg; 200 mg/kg; 400 mg/kg
Administration:

p.o.; daily; 7 days
Result:

Caused no mortality, significant changes in vital signs, or organ structure/morphology abnormalities in any dose group.
Induced a transient decrease in cholesterol levels in the 100 mg/kg group.
Led to an increase in potassium levels after 7 days of withdrawal from 400 mg/kg treatment.

Chemical Information

CAS. Nr. 3053857-55-6
Appearance Solid
Molecular Weight 515.44
Formel C₂₅H₂₀F₃N₃O₆
Color White to off-white
SMILES

O=C1N(CC2=C1C=CC(CNC(C3=CC4=C(OC3)C=CC(OC(F)(F)F)=C4)=O)=C2)C5CCC(NC5=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (194.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9401 mL

9.7004 mL

19.4009 mL

5 mM

0.3880 mL

1.9401 mL

3.8802 mL

10 mM

0.1940 mL

0.9700 mL

1.9401 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (9.70 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (9.70 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang Y, et al. Design and Discovery of Preclinical Candidate LYG-409 as a Highly Potent and Selective GSPT1 Molecular Glue Degraders. Journal of medicinal chemistry. 2025 Feb 13;68(3):2608-2638. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9401 mL	9.7005 mL	19.4009 mL	48.5023 mL
	5 mM	0.3880 mL	1.9401 mL	3.8802 mL	9.7005 mL
	10 mM	0.1940 mL	0.9700 mL	1.9401 mL	4.8502 mL
	15 mM	0.1293 mL	0.6467 mL	1.2934 mL	3.2335 mL
	20 mM	0.0970 mL	0.4850 mL	0.9700 mL	2.4251 mL
	25 mM	0.0776 mL	0.3880 mL	0.7760 mL	1.9401 mL
	30 mM	0.0647 mL	0.3233 mL	0.6467 mL	1.6167 mL
	40 mM	0.0485 mL	0.2425 mL	0.4850 mL	1.2126 mL
	50 mM	0.0388 mL	0.1940 mL	0.3880 mL	0.9700 mL
	60 mM	0.0323 mL	0.1617 mL	0.3233 mL	0.8084 mL
	80 mM	0.0243 mL	0.1213 mL	0.2425 mL	0.6063 mL
	100 mM	0.0194 mL	0.0970 mL	0.1940 mL	0.4850 mL

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LYG-409

Alle Eukaryotic Release Factor (eRF) Isoform-spezifische Produkte anzeigen