Art. -Nr.: HY-12494

LDC1267

10 Cited Publications

Kundenbewertung

Based on 10 publication(s) in Google Scholar

LDC1267 is a AXL/TAM/FLT3 inhibitor with IC₅₀ values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia.

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Reinheit: 99.64%
CAS. Nr.: 1361030-48-9
Formel: C₃₀H₂₆F₂N₄O₅
Molecular Weight:560.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LDC1267 Chemical Structure

CAS. Nr.: 1361030-48-9

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Axl

42 nM (IC₅₀)

MERTK

130 nM (IC₅₀)

Tyro3

63 nM (IC₅₀)

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Hs-578T	IC₅₀	19 nM Compound: 7; LDC1267	Inhibition of AXL in human Hs578t cells by homogeneous time-resolved fluorescence assay Inhibition of AXL in human Hs578t cells by homogeneous time-resolved fluorescence assay	[PMID: 26555154]

In Vitro

LDC1267 inhibits purified AXL, MERTK, and TYRO3 kinases with IC₅₀ values of 42 nM, 130 nM, and 63 nM, respectively, and weakly inhibits purified FLT3 kinase with an IC₅₀ of 2500 nM^[1].
LDC1267 (0.005-1 μmol/L; 30 min pre-incubation) potently and specifically inhibits GAS6-mediated AXL, AKT, and ERK1/2 phosphorylation in glioblastoma LN229 cells with IC₅₀ values of 26, 25, and 48 nmol/L, respectively^[2].
LDC1267 (up to 10 μmol/L; 72 h) does not impair the viability of glioblastoma LN229 cells at concentrations up to 10 μmol/L^[2].
LDC1267 (1-2.5 μmol/L; 4 days) specifically inhibits GAS6-induced invasion of glioblastoma LN229 spheroids at 1 and 2.5 μmol/L without reducing 2D cell viability^[2].
LDC1267 (2.5 μmol/L; 24 h) does not disrupt the endo-lysosomal compartment in wild-type or AXL KO glioblastoma LN229 cells at 2.5 μmol/L^[2].
LDC1267 (2.5 μmol/L; 24 h) does not impair autophagic flux in wild-type or AXL KO glioblastoma LN229 cells at 2.5 μmol/L^[2].
LDC1267 (1-5 μM; 72 h) potently inhibits proliferation of K562-S and K562-R cells with IC₅₀ values of 5 μM and 3 μM, respectively, in a dose-dependent manner^[3].
LDC1267 (4 μM for K562-S, 3 μM for K562-R, 4 μM combined with 0.25 μM Imatinib for K562-S; 72 h) interferes with the Wnt/β-catenin pathway in K562-S and K562-R cells by downregulating pathway regulators AXL-RTK and EYA3, and downstream targets c-Myc and Axin2, with enhanced effects when combined with Imatinib in K562-S cells^[3].
LDC1267 (4 μM; 72 h) does not induce apoptosis in K562-S or K562-R cells^[3].

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

Western Blot Analysis^[2]

Cell Line:

glioblastoma LN229 cells
Concentration:

0.005-1 μmol/L (30-minute pre-incubation); 400 ng/mL GAS6 (10-minute stimulation)
Incubation Time:

30 min (pre-incubation with LDC1267); 10 min (stimulation with GAS6)
Result:

Potently blocked GAS6-induced phosphorylation of AXL, AKT, and ERK1/2.
Displayed IC₅₀ values of 26 nmol/L for inhibition of AXL phosphorylation, 25 nmol/L for inhibition of AKT phosphorylation, and 48 nmol/L for inhibition of ERK1/2 phosphorylation.
Inhibited phosphorylation of AXL, AKT, and ERK1/2 at closely matched concentrations, indicating specificity for AXL-mediated signaling.

Cell Invasion Assay^[2]

Cell Line:

glioblastoma LN229 cells grown as spheroids
Concentration:

1-2.5 μmol/L
Incubation Time:

4 days (with GAS6)
Result:

Blocked GAS6-induced invasion of LN229 spheroids at both tested concentrations.
Did not affect the viability of 2D monolayer cultures of LN229 cells at these concentrations.

Immunofluorescence^[2]

Cell Line:

wild-type and AXL KO glioblastoma LN229 cells
Concentration:

2.5 μmol/L
Incubation Time:

24 h
Result:

Did not trigger changes in the distribution, number, or area of EEA1-positive early endosomes or LAMP1-positive late endosomes/lysosomes in either wild-type or AXL KO LN229 cells.

Cell Proliferation Assay^[3]

Cell Line:

Imatinib-sensitive K562 (K562-S), Imatinib-resistant K562 (K562-R)
Concentration:

1-5 μM
Incubation Time:

72 h
Result:

Exhibited a significant dose-dependent antiproliferative effect in both K562-S and K562-R cells.
Reached an IC₅₀ of 5 μM in K562-S cells and 3 μM in K562-R cells.

RT-PCR^[3]

Cell Line:

Imatinib-sensitive K562 (K562-S), Imatinib-resistant K562 (K562-R)
Concentration:

4 μM (K562-S cells); 3 μM (K562-R cells); 4 μM LDC1267 combined with 0.25 μM Imatinib (K562-S cells)
Incubation Time:

72 h
Result:

Significantly downregulated AXL-RTK (p-value 0.0005), EYA3 (p-value <0.0001), c-Myc (p-value <0.0001), and Axin2 (p-value <0.0001) in K562-S cells when used alone.
Caused further significant downregulation of AXL-RTK, EYA3, c-Myc, and Axin2 (p-values <0.0001) in K562-S cells when combined with Imatinib.
Significantly downregulated AXL-RTK (p-value <0.0001), EYA3 (p-value 0.0001), c-Myc (p-value <0.05), and Axin2 (p-value <0.0001) in K562-R cells.

In Vivo

Animal Model:

C57BL/6J wild type mice (8-12 weeks old syngeneic bearing B16F10 cells)^[1]
Dosage:

20mg/kg
Administration:

Intraperitoneal injection; every 12 hours for 14 days
Result:

Markedly reduced metastatic spreading of melanomas.

Chemical Information

CAS. Nr. 1361030-48-9
Appearance Solid
Molecular Weight 560.55
Formel C₃₀H₂₆F₂N₄O₅
Color White to off-white
SMILES

FC1=CC(NC(C2=NN(C3=CC=C(F)C=C3C)C=C2OCC)=O)=CC=C1OC4=CC=NC5=CC(OC)=C(OC)C=C54
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

All WB

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Journal Impact Factor

Cancer Cell

Adiponectin reduces immune checkpoint inhibitor-induced inflammation without blocking anti-tumor immunity. [Abstract]

2025 Feb 10;43(2):269-291.e19. PMID: 39933899
Theranostics

Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]

2018 Jul 30;8(15):4262-4278. PMID: 30128052

LDC1267 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]

BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

LDC1267 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]

BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.
Cell Commun Signal

Bisecting GlcNAc modification of vesicular GAS6 regulates CAFs activation and breast cancer metastasis. [Abstract]

2025 Jan 22;23(1):39. PMID: 39844194
Cell Mol Life Sci

Endocytic trafficking of GAS6-AXL complexes is associated with sustained AKT activation. [Abstract]

2022 May 27;79(6):316. PMID: 35622156
J Mol Med (Berl)

Sex hormone-binding globulin restrains hepatic fibrosis via inhibition of Tgfβ expression. [Abstract]

2025 Sep;103(9):1043-1053. PMID: 40616670
FEBS J

TNF-α/ENO1 signaling facilitates testicular phagocytosis by directly activating Elmo1 gene expression in mouse Sertoli cells. [Abstract]

2022 May;289(10):2809-2827. PMID: 34919331
Biology (Basel)

Alcohol and HIV-Derived Hepatocyte Apoptotic Bodies Induce Hepatic Stellate Cell Activation. [Abstract]

2022 Jul 14;11(7):1059. PMID: 36101437
Nencki Institute of Experimental Biology

2022 Oct.
Universität Würzburg

2022 Feb.
bioRxiv

2020 Mar.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (89.20 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

1.7840 mL

8.9198 mL

17.8396 mL

5 mM

0.3568 mL

1.7840 mL

3.5679 mL

10 mM

0.1784 mL

0.8920 mL

1.7840 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (4.46 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 (4.46 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. 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 (4.46 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 10 mg/mL (17.84 mM); Suspended solution; Need ultrasonic

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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Chakrabarti A, et al. Exploring the functions of TAM kinases: Assay development and characterization of potential therapeutics[C]//Molecular Cancer Therapeutics. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2018, 17(1).

[2]. Zdżalik-Bielecka D, et al. Bemcentinib and Gilteritinib Inhibit Cell Growth and Impair the Endo-Lysosomal and Autophagy Systems in an AXL-Independent Manner. Mol Cancer Res. 2022;20(3):446-455. [Content Brief]

[3]. Yousaf M, et al. TAM family kinases are potential candidate targets for therapeutic intervention in chronic myeloid leukemia. Discov Oncol. 2025;16(1):1944. Published 2025 Oct 21. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7840 mL	8.9198 mL	17.8396 mL	44.5991 mL
	5 mM	0.3568 mL	1.7840 mL	3.5679 mL	8.9198 mL
	10 mM	0.1784 mL	0.8920 mL	1.7840 mL	4.4599 mL
	15 mM	0.1189 mL	0.5947 mL	1.1893 mL	2.9733 mL
	20 mM	0.0892 mL	0.4460 mL	0.8920 mL	2.2300 mL
	25 mM	0.0714 mL	0.3568 mL	0.7136 mL	1.7840 mL
	30 mM	0.0595 mL	0.2973 mL	0.5947 mL	1.4866 mL
	40 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1150 mL
	50 mM	0.0357 mL	0.1784 mL	0.3568 mL	0.8920 mL
	60 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL
	80 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5575 mL

Keywords

LDC1267

10 Cited Publications

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LDC1267

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDC1267

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDC1267

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDC1267

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDC1267 Related Classifications

HY-12494 Related Classifications