Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 30.00 | |
2 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 70.00 | |
10 mg | In stock | $ 107.00 | |
25 mg | In stock | $ 177.00 | |
50 mg | In stock | $ 261.00 | |
100 mg | In stock | $ 441.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 85.00 |
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). |
Targets&IC50 | Tyro3:8 nM, Mer:<5 nM, Axl:29 nM |
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. |
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. |
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) |
Molecular Weight | 560.55 |
Formula | C30H26F2N4O5 |
CAS No. | 1361030-48-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (165.9 mM)
Ethanol: 2 mg/mL (3.56 mM), Heating is recommended.
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LDC1267 1361030-48-9 Tyrosine Kinase/Adaptors TAM Receptor LDC-1267 LDC 1267 Tyro3 Inhibitor inhibit Axl Mer inhibitor