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| 50mg |
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| 100mg |
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(±)-Zanubrutinib is a racemic mixture of Zanubrutinib (formerly known as BGB-3111) which is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers. BGB-3111 showed nanomolar BTK inhibition activity in both biochemical and cellular assays. BGB-3111 effectively suppressed BCR aggregation-induced BTK autophosphorylation, obstructed downstream PLC-γ2 signaling, and slowed down the growth of multiple MCL and DLBCL cell lines. Against a panel of kinases, including ITK, BGB-3111 exhibited far more restricted off-target activities in contrast to ibrutinib. BGB-3111 was at least ten times less effective than ibrutinib in inhibiting rituximab-induced ADCC, which is consistent with its weak ITK inhibition activity. However, ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells.
| ln Vitro |
(±)-Zanubrutinib ((±)-BGB-3111) exhibits nanomolar Btk inhibition activity in both biochemical and cellular assays. (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation in a number of MCL and DLBCL cell lines. When it comes to a panel of kinases, including ITK, (±)-Zanubrutinib exhibits far more limited off-target activities when compared to PCI-32765[1].
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| ln Vivo |
(±)-Zanubrutinib produces dose-dependent anti-tumor effects against REC-1 MCL xenografts that are injected into mice's tail veins and engrafted subcutaneously or systemically. in the xenografts placed beneath the skin. An initial 14-day rat toxicity study reveals that (±)-Zanubrutinib is highly well tolerated, and doses up to 250 mg/kg/day do not result in the maximal tolerated dose (MTD) being reached[1].
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| References |
| Molecular Formula |
C27H29N5O3
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| Molecular Weight |
471.56
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| Exact Mass |
471.2270398
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| CAS # |
1633350-06-7
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| Related CAS # |
Zanubrutinib;1691249-45-2;(R)-Zanubrutinib;1691249-44-1;Zanubrutinib-d5
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| Appearance |
Solid
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| SMILES |
C=CC(=O)N1CCC(CC1)C2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N
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| InChi Key |
RNOAOAWBMHREKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29N5O3/c1-2-23(33)31-16-13-18(14-17-31)22-12-15-29-27-24(26(28)34)25(30-32(22)27)19-8-10-21(11-9-19)35-20-6-4-3-5-7-20/h2-11,18,22,29H,1,12-17H2,(H2,28,34)
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| Chemical Name |
2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1206 mL | 10.6031 mL | 21.2062 mL | |
| 5 mM | 0.4241 mL | 2.1206 mL | 4.2412 mL | |
| 10 mM | 0.2121 mL | 1.0603 mL | 2.1206 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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