LDC1267TAM kinase inhibitor,highly selective CAS# 1361030-48-9 |
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Quality Control & MSDS
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| Cas No. | 1361030-48-9 | SDF | Download SDF |
| PubChem ID | 56847486 | Appearance | Powder |
| Formula | C30H26F2N4O5 | M.Wt | 560.55 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (89.20 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide | ||
| 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 | ||
| Standard InChIKey | ISPBCAXOSOLFME-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.
IC50 value: <5 nM/8 nM/29 nM(Tyro3/Axl/Mer) [1]
Target: TAM kinase inhibitor
in vitro: LDC1267 preferentially inhibits Tyro3,Axl andMer at lownanomolarity, as determined by tracer-based binding assays. Treatment of NKG2D activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation;LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells.
in vivo: wild-type mice treated with LDC1267 showed enhanced cytotoxicity towardsRMAcells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. Challenged mice with B16F10 melanoma followed
by intraperitoneal LDC1267 treatment. LDC1267 markedly reduced metastatic spreading ofmelanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267. References: | |||||
LDC1267 Dilution Calculator
LDC1267 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.784 mL | 8.9198 mL | 17.8396 mL | 35.6792 mL | 44.5991 mL |
| 5 mM | 0.3568 mL | 1.784 mL | 3.5679 mL | 7.1358 mL | 8.9198 mL |
| 10 mM | 0.1784 mL | 0.892 mL | 1.784 mL | 3.5679 mL | 4.4599 mL |
| 50 mM | 0.0357 mL | 0.1784 mL | 0.3568 mL | 0.7136 mL | 0.892 mL |
| 100 mM | 0.0178 mL | 0.0892 mL | 0.1784 mL | 0.3568 mL | 0.446 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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LDC1267 is a highly selective TAM kinase inhibitor with IC50 of < 5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively.
LDC1267 preferentially inhibits Tyro3, Axl and Mer at low nano-molarity by tracer-based binding assays. Treatment of NKG2D- activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation; LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. Adoptive transfer of LDC1267-treated wild-type NK cells significantly increased the anti-tumour response to levels observed in mice transplanted with Cbl-b2/2 NK cells, but did not increase the anti-metastatic efficacy of Cbl-b-knockout NK cells, reinforcing the notion that Cbl-b acts downstream of TAM receptors for NK cell inhibition. [1]
In vivo, wild-type mice treated with LDC1267 showed enhanced cytotoxicity towards RMA cells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. LDC1267 markedly reduced metastatic spreading of melanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267. LDC1267 treatment significantly reduced the numbers and sizes of 4T1 micro-metastases in the liver, without any apparent effect on the primary vehicle LDC1267 mammary tumor. NK cell depletion using anti-asialoGM1 antibodies resulted in markedly enhanced 4T1 liver metastases and abolished the therapeutic benefits of LDC1267. Oral LDC1267 significantly reduced 4T1 liver micro-metastases. [1]
References:
[1]. Paolino M, Choidas A2, Wallner S et al. The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12. doi: 10.1038/nature12998. Epub 2014 Feb 19.
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