Art. -Nr.: HY-162540

LLC355

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LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader with a DC₅₀ of 150.8 nM. LLC355 induces DDR1 protein degradation via lysosome-mediated autophagy. LLC355 inhibits the tumorigenicity, migration and invasion abilities of cancer cells, and induces apoptosis. LLC355 is applicable to research related to non-small cell lung cancer and pancreatic cancer.
(Pink: DDR1 Target protein ligand; Blue: LC3 ligand (HY-50759); Black: linker).

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Reinheit: 99.71%
Formel: C₆₃H₆₄ClF₃N₁₀O₅
Molecular Weight:1133.69

Speicherung:

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

LLC355 Chemical Structure

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader with a DC₅₀ of 150.8 nM. LLC355 induces DDR1 protein degradation via lysosome-mediated autophagy. LLC355 inhibits the tumorigenicity, migration and invasion abilities of cancer cells, and induces apoptosis. LLC355 is applicable to research related to non-small cell lung cancer and pancreatic cancer^[1]. (Pink: DDR1 Target protein ligand; Blue: LC3 ligand (HY-50759); Black: linker).

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

In Vitro

Compound LLC355 (0.3-10000 nM; 1-24 h) dose- and time-dependently degrades DDR1 protein in NCI-H23 cells with a DC₅₀ of 150.8 nM, without altering DDR2 levels^[1].
Compound LLC355 (0.3 μM; 24 h) potently inhibits migration and invasion of NCI-H23 cells and reduces N-cadherin expression^[1].
Compound LLC355 (0.1-1 μM; 10 days) potently suppresses colony formation of NCI-H23 cells over 10 days, with greater potency than DDR1 inhibitor 1^[1].
Compound LLC355 (100-1000 nM; 24 h) does not induce apoptosis in NCI-H23 cells at 0.3 μM after 24 h treatment, but induces apoptosis at 1 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H23
Concentration:

0.3 μM (24 h); 1 μM (24 h); 1-10000 nM (12 h); 1 μM (1 h, 3 h, 6 h, 12 h, 24 h)
Incubation Time:

1 h, 3 h, 6 h, 12 h, 24 h
Result:

Induced 40% DDR1 degradation at 0.3 μM after 24 h treatment.
Induced 92% DDR1 degradation at 1 μM after 24 h treatment.
Dose-dependently degraded DDR1 with a DC₅₀ value of 150.8 nM after 12 h treatment.
Time-dependently degraded DDR1 with maximal degradation observed at 24 h when treated with 1 μM.
Did not affect DDR2 protein levels at evaluated concentrations.

Cell Migration Assay ^[1]

Cell Line:

PANC-1, MIA-PaCa-2
Concentration:

0.3 and 1 μM
Incubation Time:

24 h
Result:

Inhibited cell migration.

Cell Invasion Assay^[1]

Cell Line:

PANC-1, MIA-PaCa-2
Concentration:

0.3 and 1 μM
Incubation Time:

24 h
Result:

Inhibited cell invasion.

Western Blot Analysis^[1]

Cell Line:

PANC-1, MIA-PaCa-2
Concentration:

0.1, 0.3 and 1 μM
Incubation Time:

24 h
Result:

Down-regulated the expression of N-Cadherin protein in a concentration-dependent manner.
Induced PARP cleavage in a concentration-dependent manner (i.e., promotes cell apoptosis).

Cell Proliferation Assay^[1]

Cell Line:

NCI-H23
Concentration:

0.1, 0.3 and 1 μM
Incubation Time:

10 days
Result:

Potently suppressed colony formation in NCI-H23 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	F	CL
Rat^[1]	2 mg/kg	i.v.	3.18 h	0.08 h	27019.53 ng/mL	30094.61	/	66.67 mL/h/kg
Rat^[1]	10 mg/kg	p.o.	3.99 h	3.33 h	226.36 ng/mL	1151.55 ng·h/mL	0.77 %	/

Chemical Information

Appearance Solid
Molecular Weight 1133.69
Formel C₆₃H₆₄ClF₃N₁₀O₅
Color White to light yellow
SMILES

O=C1C2=CC=C(Cl)C=C2N=C([C@H](N(C(C3=CC=C(C)C=C3)=O)CCCNC(COCCN4CCN(CC5=CC(C(F)(F)F)=CC(NC(C6=CC(C#CC(C=N7)=CN8C7=CC=N8)=C(CC)C=C6)=O)=C5)CC4)=O)C(C)C)N1CC9=CC=CC=C9
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (88.21 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

0.8821 mL

4.4104 mL

8.8208 mL

5 mM

0.1764 mL

0.8821 mL

1.7642 mL

10 mM

0.0882 mL

0.4410 mL

0.8821 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: ≥ 2.5 mg/mL (2.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.21 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (2.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Liu L, et al. Discovery of as an Autophagy-Tethering Compound for the Degradation of Discoidin Domain Receptor 1. Journal of medicinal chemistry. 2024 May 23;67(10):8043-8059. [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	0.8821 mL	4.4104 mL	8.8208 mL	22.0519 mL
	5 mM	0.1764 mL	0.8821 mL	1.7642 mL	4.4104 mL
	10 mM	0.0882 mL	0.4410 mL	0.8821 mL	2.2052 mL
	15 mM	0.0588 mL	0.2940 mL	0.5881 mL	1.4701 mL
	20 mM	0.0441 mL	0.2205 mL	0.4410 mL	1.1026 mL
	25 mM	0.0353 mL	0.1764 mL	0.3528 mL	0.8821 mL
	30 mM	0.0294 mL	0.1470 mL	0.2940 mL	0.7351 mL
	40 mM	0.0221 mL	0.1103 mL	0.2205 mL	0.5513 mL
	50 mM	0.0176 mL	0.0882 mL	0.1764 mL	0.4410 mL
	60 mM	0.0147 mL	0.0735 mL	0.1470 mL	0.3675 mL
	80 mM	0.0110 mL	0.0551 mL	0.1103 mL	0.2756 mL

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LLC355

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LLC355 Related Classifications

HY-162540 Related Classifications