Product Details
Product Name:
LDC1267 |
CAS No.:
1361030-48-9 |
Purity:
99.76% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | LDC1267 |
Description | LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM). |
Cell Research | After incubation for 72?hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.(Only for Reference) |
Kinase Assay | Kinase binding assays: For optimization of Axl/TAM receptor inhibitors, an Axl binding assay is established (HTRF method; Kinase tracer 236). This assay is based on the binding and displacement of the Alexa Fluor 647-labelled Kinase tracer 236 to each glutathione S-transferase (GST)-tagged kinase used in the binding assay. Binding of the tracer to the kinase was detected by using europium (Eu)-labelled anti-GST antibodies. Simultaneous binding of both the fluorescent tracer and the Eu-labelled antibodies to the GST-tagged kinase generates a fluorescence resonance energy transfer (FRET) signal. Binding of inhibitor to the kinase competes for binding with the tracer, resulting in a loss of the FRET signal. For the assay, the compound is diluted in 20?mM HEPES, pH?8.0, 1?mM DTT, 10?mM MgCl2 and 0.01% Brij35. Then, the kinase of interest (5?nM final concentration), fluorescent tracer (15?nM final concentration) and LanthaScreen Eu-anti-GST antibody (2?nM final concentration) are mixed with the respective compound dilutions (from 5?nM to 10?μM) and incubated for 1?h. The FRET signal is quantified using an EnVision Multilabellreader 2104. |
In vitro | In mice bearing B16F10 melanoma, intraperitoneal injection of LDC1267 (20 mg/kg) exhibits high safety and is capable of inhibiting tumor metabolism and enhancing the activity of anti-metastatic NK cells. |
In vivo | In various cell lines, LDC1267 exhibits inhibition of cellular proliferation with an IC50 >5 μM. Moreover, in NKG2D-activated NK cells, LDC1267 can block the inhibitory effect induced by Gas6 stimulation. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 93 mg/mL (165.9 mM) Ethanol : 2 mg/mL (3.56 mM), Heating is recommended.
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Keywords | LDC-1267 | LDC 1267 | Tyro3 | LDC1267 | Inhibitor | inhibit | TAM Receptor | Axl | Mer |
Inhibitors Related | UNC2025 | Cabozantinib | Gilteritinib | Bemcentinib | SGI-7079 | Dubermatinib | Sitravatinib | NCT-503 | Cabozantinib S-malate | AXL-IN-13 | G-749 | BMS 777607 |
Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |