LDC1267

Alias: LDC-1267; LDC1267; LDC 1267
Cat No.:V0638 Purity: ≥98%
LDC1267 (LDC-1267) is a novel, highly potent and selective TAM (Tyro3, Axl and Mer) kinase inhibitor with potential antitumor activity.
LDC1267 Chemical Structure CAS No.: 1361030-48-9
Product category: TAM Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

LDC1267 (LDC-1267) is a novel, highly potent and selective TAM (Tyro3, Axl and Mer) kinase inhibitor with potential antitumor activity. It has lower effects on other kinases like Met, Aurora B, Lck, Src, and CDK8, and inhibits Mer, Tyro3, and Axl with IC50s of<5 nM, 8 nM, and 29 nM, respectively. In the mouse B16F10 metastatic melanoma model, it exhibits outstanding in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
Targets
Mer (IC50 <5 nM); Tyro3 (IC50 = 8 nM); Axl (IC50 = 29 nM)
ln Vitro

LDC1267 has an IC50 of >5μM and reasonably inhibits the growth of 11 out of 95 distinct cell lines. Gas6 stimulation's inhibitory effects are eliminated by LDC1267 in NKG2D-activated NK cells.[1]

ln Vivo
LDC1267 (20 mg/kg, i.p.) effectively increases anti-metastatic NK cell activity in B16F10 melanoma-bearing mice and rejects tumor metastases without causing significant cytotoxicity.[1]
Enzyme Assay
Kinase tracer 236 and the HTRF method have established an Axl binding assay for the purpose of optimizing Axl/TAM receptor inhibitors. The basis of this assay is the binding and displacement of each glutathione S-transferase (GST)-tagged kinase utilized in the binding assay by the Alexa Fluor 647-labelled Kinase tracer 236, as demonstrated by this method. Utilizing anti-GST antibodies labeled with europium (Eu), the tracer's binding to the kinase was distinguished. A fluorescence resonance energy transfer (FRET) signal is produced when the fluorescent tracer and the Eu-labeled antibodies bind to the GST-tagged kinase simultaneously. The FRET signal is lost when the inhibitor binds to the kinase and competes with the tracer for binding. The chemical is diluted in 20 mM HEPES, pH 8.0, 1 mM DTT, 10 mM MgCl2, and 0.01% Brij35 for the assay. Next, the compound dilutions ranging from 5 nM to 10 μM are combined with the kinase of interest (5 nM final concentration), fluorescent tracer (15 nM final concentration), and LanthaScreen Eu-anti-GST antibody (2 nM final concentration) and incubated for a duration of 1 hour. An EnVision Multilabellreader 2104 is used to quantify the FRET signal.
Cell Assay
CellTiterGlow reagent is used to measure the proliferation in comparison to the corresponding DMSO control after the LDC1267 is incubated for 72 hours.
Animal Protocol
Mouse B16F10 metastatic melanoma model
20 mg/kg
i.p.
References

[1]. Nature . 2014 Mar 27;507(7493):508-12.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H26F2N4O5
Molecular Weight
560.55
Exact Mass
560.560
Elemental Analysis
C, 64.28; H, 4.68; F, 6.78; N, 10.00; O, 14.27
CAS #
1361030-48-9
Appearance
Solid powder
SMILES
CCOC1=CN(N=C1C(=O)NC2=CC(=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)F)C5=C(C=C(C=C5)F)C
InChi Key
ISPBCAXOSOLFME-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H26F2N4O5/c1-5-40-28-16-36(23-8-6-18(31)12-17(23)2)35-29(28)30(37)34-19-7-9-25(21(32)13-19)41-24-10-11-33-22-15-27(39-4)26(38-3)14-20(22)24/h6-16H,5H2,1-4H3,(H,34,37)
Chemical Name
N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide
Synonyms
LDC-1267; LDC1267; LDC 1267
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~178.4 mM)
Water: <1 mg/mL
Ethanol: ~2 mg/mL (~3.6 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • LDC1267

    a, TC-1 tumour growth in Cbl-b+/+ Rag2−/− and Cbl-b−/− Rag2−/− mice (mean ± s.e.m., n = 10 each). ***P 

  • LDC1267

    a, In vitro Cbl-b-dependent ubiquitylation of Tyro3, Axl and Mer (anti-Ub). Control, no TAM receptors. Loading controls are shown. b, IFN-γ+ Cbl-b+/− and Cbl-b−/− NK cells (%) stimulated with anti-NKG2D antibodies in the presence of sol…Nature. 2014 Mar 27;507(7493):508-12.

  • LDC1267

    a, Kinetics of primary 4T1 tumour cell growth in the mammary fat pad of control and anti-asialo GM1-treated mice that received LDC1267 or vehicle (mean ± s.e.m., n = 6–9 mice per group). NS, not significant (one-way ANOVA). Nature. 2014 Mar 27;507(7493):508-12.

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