Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 0.18 μM (BTK)[1]
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ln Vitro |
Cys481 may play a role in how Elsubrutinib inhibits BTK, as Elsubrutinib inhibits BTK (C481S) with an IC50 of 2.6 μM, indicating a significant loss in potency upon exchanging the targeted thiol nucleophile with an alcohol. Elsubrutinib prevents BTK-dependent cellular activation and BTK enzyme activity irreversibly. Elsubrutinib blocks the release of histamine from basophils stimulated by IgE and IL-6 from monocytes stimulated by IgG, which use the Fce and Fcc receptors, respectively. Elsubrutinib inhibits IgM-mediated B cell proliferation, which is dependent on signaling through the BCR. Elsubrutinib also prevents TNF from being released from PBMCs stimulated by CpG-DNA, which is signaled through TLR9. However, it has no effect on TLRs that do not use ITAM motifs, such as TLR4 (which is stimulated with LPS) or TLR7/8 (which is stimulated with R848). Elsubrutinib significantly affects the proliferation of B cells mediated by IgM[1].
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ln Vivo |
Antibody responses to NP-Ficoll and NP-KLH are inhibited by elsubrutinib (10 mg/kg; po), but not to NP-LPS or Prevnar-13[1]. At 10 mg/kg QD and BID doses, elsubrutinib (0.1~10 mg/kg; po) effectively delays the start of proteinuria, prolongs survival, and inhibits paw edema throughout the course of the disease; lower doses do not appreciably inhibit these endpoints[1]. Paw volume gains are shown to be exposure-dependently inhibited by elsubrutinib. Elsubrutinib substantially reduces bone volume loss in a dose-dependent manner that is in line with the anti-inflammatory effects that have been noted[1].
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Animal Protocol |
Animal/Disease Models: Female C57/BL6 mice[1]
Doses: 10 mg/kg Route of Administration: Po Experimental Results: Inhibited antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13. Animal/Disease Models: Lewis rats[1] Doses: 0.1~10 mg/kg Route of Administration: Po Experimental Results: Resulted in dose-dependent inhibition of paw swelling throughout the course of disease. Animal/Disease Models: NZBWF1 mice[1] Doses: 0.1~10 mg/kg Route of Administration: Po Experimental Results: Dramatically prevented the onset of proteinuria and prolonged survival at the 10 mg/kg QD and BID doses , while lower doses did not Dramatically inhibit these endpoints. |
References |
[1]. Goess C, et al. ABBV-105, a selective and irreversible inhibitor of Bruton's tyrosine kinase, is efficacious in multiple preclinical models of inflammation [published correction appears in Mod Rheumatol. 2019 May;29(3):v]. Mod Rheumatol. 2019;29(3):510-52
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Molecular Formula |
C17H19N3O2
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Molecular Weight |
297.35
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CAS # |
1643570-24-4
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Related CAS # |
(R)-Elsubrutinib;1643570-23-3
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SMILES |
C1(=CC=C([C@H]2CN(C(C=C)=O)CCC2)C2=C1NC=C2)C(N)=O
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | |
5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | |
10 mM | 0.3363 mL | 1.6815 mL | 3.3630 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.