| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
QL47R is designed to be a selective inactive analogue; it lacks significant inhibitory activity against BTK. While QL47 inhibits BTK with an IC₅₀ of ~1 nM, QL47R has an IC₅₀ >10 µM (>10,000‑fold reduction). It also does not bind covalently to the Cys481 residue. However, it may retain some non‑specific binding to other kinases or proteins, which makes it a useful tool for assessing the specificity of QL47. Its target is essentially "none" in the context of BTK, but it serves as a specificity control in cellular and biochemical assays.
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| ln Vitro |
In vitro, QL47R shows no significant inhibition of BTK kinase activity in enzymatic assays at concentrations up to 10 µM. In B‑cell receptor (BCR)‑stimulated Ramos cells, QL47R does not reduce the phosphorylation of BTK or downstream PLCγ2, while QL47 completely abolishes it at 100 nM. It does not affect B‑cell proliferation or survival at concentrations up to 10 µM. It may have weak activity against other targets due to the carbazole scaffold, but these are not well characterised. It is stable in cell culture media for up to 48 h.
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| ln Vivo |
In vivo, QL47R is used as a negative control in mouse models of B‑cell lymphoma. While QL47 (10 mg/kg, IP) significantly inhibits tumour growth in xenograft models, QL47R at the same dose shows no effect on tumour volume or survival, confirming that the anti‑tumour activity of QL47 is entirely BTK‑dependent. It also does not induce apoptosis in lymphoma tissues, as assessed by cleaved caspase‑3 staining. The compound has no observable effect on plasma cytokine levels or immune cell populations.
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| Enzyme Assay |
In vitro kinase inhibition assays: BTK (recombinant human, 0.5 nM) is incubated with QL47R (0.001‑100 µM) in the presence of 10 µM ATP and a peptide substrate for 60 min. Phosphorylation is detected using an HTRF kit. The IC₅₀ is calculated. For covalent binding assessment, the compound is pre‑incubated with BTK for 30 min, then diluted 100‑fold before adding ATP; if inhibition persists (time‑dependent), covalent binding is indicated. QL47R shows no time‑dependent inhibition, unlike QL47.
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| Cell Assay |
Cell‑based assays: Ramos (Burkitt's lymphoma) cells are serum‑starved and treated with QL47R (0.01‑10 µM) for 2 h, then stimulated with anti‑IgM (10 µg/mL) for 5 min. Cell lysates are immunoblotted for pBTK (Tyr223), pPLCγ2, and total BTK. QL47R does not reduce pBTK or pPLCγ2. Cell viability is measured by CellTiter‑Glo after 72 h exposure. The EC₅₀ for cytotoxicity is >20 µM for QL47R, while QL47 is ~0.1 µM. For selectivity profiling, a panel of 50 kinases is screened at 1 µM QL47R; inhibition is <30% for all tested.
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| Animal Protocol |
In vivo experiments are performed in NSG mice bearing subcutaneous Ramos xenografts. QL47R is formulated in 10% DMSO/90% corn oil and administered intraperitoneally at 10 mg/kg once daily for 14 days. Tumour volumes are measured every 3 days. Blood is collected for PK analysis. At endpoint, tumours are excised, weighed, and processed for immunohistochemistry (Ki‑67, cleaved caspase‑3). Body weights are monitored for toxicity. QL47R shows no activity; it is used as a comparator group.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of QL47R are similar to QL47: moderate oral bioavailability (~30%), half‑life ~4‑6 h in mice, high protein binding (>90%). It is cleared by hepatic metabolism, mainly via CYP3A4. The compound distributes into tumour tissue with a tumour:plasma ratio of approximately 1.5. In mice, the Tmax is 1‑2 h. The PK profile confirms that the lack of efficacy is not due to poor exposure but due to the absence of BTK binding.
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| Toxicity/Toxicokinetics |
Toxicity of QL47R: at doses up to 20 mg/kg daily for 14 days in mice, no significant toxic effects are observed—no body weight loss, no changes in liver enzymes, and no haematological abnormalities. This is consistent with its inactivity. It is not genotoxic in Ames tests. The compound is considered safe for research use. In contrast, the active enantiomer QL47 shows some gastrointestinal toxicity at high doses, which is absent in QL47R, reinforcing its utility as a control.
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| References | |
| Additional Infomation |
Additional information: QL47R (CAS 1579278‑89‑9) is a valuable research tool for validating BTK‑specific effects. It is not a drug candidate and has no clinical development status. Its chemical synthesis yields the R enantiomer, while the active QL47 is the S enantiomer. The compound is supplied as a white solid and stored at –20°C. It is used in academic and pharmaceutical research to confirm the mechanism of action of BTK inhibitors and to rule out off‑target liabilities. No clinical trials exist for QL47R; it is exclusively a preclinical reference standard.
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| Molecular Formula |
C27H23N5O2
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| Molecular Weight |
449.50
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| CAS # |
1579278-89-9
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| Appearance |
Off-white to light yellow solid powder
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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 :~100 mg/mL (~222.47 mM; with sonication)
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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 | 2.2247 mL | 11.1235 mL | 22.2469 mL | |
| 5 mM | 0.4449 mL | 2.2247 mL | 4.4494 mL | |
| 10 mM | 0.2225 mL | 1.1123 mL | 2.2247 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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