| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
QL47 targets Bruton's tyrosine kinase (BTK) with high potency and selectivity. It inhibits BTK kinase activity with an IC₅₀ of 7 nM. The compound covalently modifies Cys481 in the kinase domain of BTK, leading to irreversible inhibition. In cells, QL47 inhibits autophosphorylation of BTK on Tyr223 with an EC₅₀ of 475 nM and inhibits phosphorylation of the downstream effector PLCγ2 (Tyr759) with an EC₅₀ of 318 nM.
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| ln Vitro |
QL47 blocks the initiation of both canonical cap-driven and noncanonical initiation strategies for protein neosynthesis, most likely by focusing on an early stage of translation elongation[2].
QL47 has an EC50 of 475 nM on autophosphorylation of BTK on Tyr223 and an EC50 of 318 nM on phosphorylation of a downstream effector, PLCγ2 (Tyr759). QL47 causes a G1 cell cycle arrest in Ramos cells, which is linked to a marked BTK protein degradation. At submicromolar concentrations, QL47 prevents B-cell lymphoma cancer cell lines from proliferating[3]. In vitro, QL47 demonstrates potent inhibition of BTK kinase activity with an IC₅₀ of 7 nM. It inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations. The compound's irreversible binding to BTK provides sustained target inhibition, and its selectivity for BTK over other kinases contributes to its favorable profile. |
| ln Vivo |
In vivo, QL47 has been evaluated in preclinical models of B-cell malignancies. As a BTK inhibitor, it has the potential to inhibit B-cell receptor signaling and reduce tumor growth. The compound's irreversible binding and potent activity support its investigation for oncology and antiviral applications.
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| Enzyme Assay |
In vitro enzyme assays for BTK inhibition involve incubating recombinant BTK kinase with a peptide substrate and ATP in the presence of varying concentrations of QL47. Kinase activity is measured using radioactive, fluorescence-based, or luminescent assays. IC₅₀ values are calculated from dose-response curves to determine the compound's potency.
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| Cell Assay |
Cellular assays are performed using B-cell lymphoma cell lines such as Ramos cells. Cells are treated with QL47 at various concentrations for 1-72 hours. BTK autophosphorylation at Tyr223 is assessed by Western blot using phospho-specific antibodies. PLCγ2 phosphorylation at Tyr759 is measured to confirm downstream signaling inhibition. Cell proliferation is evaluated by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo studies are conducted in xenograft mouse models of B-cell malignancies. QL47 is administered orally or intraperitoneally at various doses. Tumor volume is measured periodically, and tumors are harvested for biomarker analysis, including assessment of phospho-BTK and Ki-67 by immunohistochemistry.
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| ADME/Pharmacokinetics |
QL47 (molecular weight 447.48, formula C₂₇H₂₁N₅O₂) is a small-molecule compound. It is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of QL47 have been limited, as the compound is primarily used as a research tool. As a BTK inhibitor, its toxicity profile is related to inhibition of B-cell function. No significant toxicity has been reported in the available literature.
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| References |
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| Additional Infomation |
9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxopropyl-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthidium is a naphthidine derivative.
QL47 (QL-XII-47) is a potent and selective irreversible BTK inhibitor. Its mechanism involves covalent modification of Cys481 in BTK, leading to irreversible inhibition of BTK kinase activity and suppression of BCR signaling. The compound inhibits B-cell lymphoma proliferation at submicromolar concentrations. QL47 is primarily used for research purposes and has not received regulatory approval for clinical use. |
| Molecular Formula |
C27H21N5O2
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|---|---|
| Molecular Weight |
447.487945318222
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| Exact Mass |
447.169
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| Elemental Analysis |
C, 72.47; H, 4.73; N, 15.65; O, 7.15
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| CAS # |
1469988-75-7
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| Related CAS # |
1469988-75-7
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| PubChem CID |
71748056
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| Appearance |
white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
706.2±60.0 °C at 760 mmHg
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| Flash Point |
380.9±32.9 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.724
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
34
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| Complexity |
860
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C2=C(C=C1)C=NC3=CC=C(C4=CN(C)N=C4)C=C32)C5=CC=C(CC6)C(N6C(C=C)=O)=C5
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| InChi Key |
RTRNJQOBEOISFQ-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
9-(1-methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-one
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| Synonyms |
QL47; QL 47; QL47; QL-XII 47; QL-XII-47; QL XII-47
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~1 mg/mL (~2.2 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2347 mL | 11.1734 mL | 22.3469 mL | |
| 5 mM | 0.4469 mL | 2.2347 mL | 4.4694 mL | |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2347 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.
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.
(2) Be sure to add the solvent(s) in order.
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