QL47

BTK kinase inhibitor CAS# 1469988-75-7

QL47

2D Structure

Catalog No. BCC3920----Order now to get a substantial discount!

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Quality Control of QL47

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QL47

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Chemical Properties of QL47

Cas No. 1469988-75-7 SDF Download SDF
PubChem ID 71748056 Appearance Powder
Formula C27H21N5O2 M.Wt 447.49
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BTK Inhibitor
Solubility DMSO : < 1 mg/mL (insoluble or slightly soluble)
Chemical Name 9-(1-methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-one
SMILES CN1C=C(C=N1)C2=CC3=C4C(=CN=C3C=C2)C=CC(=O)N4C5=CC6=C(CCN6C(=O)C=C)C=C5
Standard InChIKey RTRNJQOBEOISFQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H21N5O2/c1-3-25(33)31-11-10-17-4-7-21(13-24(17)31)32-26(34)9-6-19-14-28-23-8-5-18(12-22(23)27(19)32)20-15-29-30(2)16-20/h3-9,12-16H,1,10-11H2,2H3
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.
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.
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.

Biological Activity of QL47

DescriptionQL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM. IC50 Value: 7 nM Target: Btk in vitro: QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest which is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations [1]. in vivo: N/A

References:
[1]. Wu, H., et al., Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol, 2014.

QL47 Dilution Calculator

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QL47 Molarity Calculator

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Preparing Stock Solutions of QL47

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2347 mL 11.1734 mL 22.3469 mL 44.6937 mL 55.8672 mL
5 mM 0.4469 mL 2.2347 mL 4.4694 mL 8.9387 mL 11.1734 mL
10 mM 0.2235 mL 1.1173 mL 2.2347 mL 4.4694 mL 5.5867 mL
50 mM 0.0447 mL 0.2235 mL 0.4469 mL 0.8939 mL 1.1173 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.4469 mL 0.5587 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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Universidade da Beira Interior

The Institute of Cancer Research

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Auckland University
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The University of Tokyo
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Korea University
Korea University

Background on QL47

QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces

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References on QL47

Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.[Pubmed:28337328]

ACS Med Chem Lett. 2017 Feb 3;8(3):344-349.

Here we report the structure-activity relationship (SAR) investigations of QL-XII-47 (QL47), a compound that possesses broad-spectrum antiviral activity against dengue virus and other RNA viruses. A medicinal chemistry campaign initiated from QL47, a previously reported covalent BTK inhibitor, to derive YKL-04-085, which is devoid of any kinase activity when screened against a panel of 468 kinases and with improved pharmacokinetic properties. Both QL47 and YKL-04-085 are potent inhibitors of viral translation and exhibit cellular antiviral activity at 35-fold lower concentrations relative to inhibition of host-cell proliferation.

Description

QL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.

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