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Purity: ≥98%
Zanubrutinib (formerly known as BGB-3111), an S-enantiomer, is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers. BGB-3111 showed evidence of nanomolar BTK inhibition activity in both biochemical and cellular assays. BGB-3111 exhibited potent inhibition of cell proliferation in multiple MCL and DLBCL cell lines, as well as blocking downstream PLC-γ2 signaling and BTK autophosphorylation triggered by BCR aggregation. BGB-3111 demonstrated far more constrained off-target activities against a panel of kinases, including ITK, when compared to ibrutinib. Ibrutinib considerably reduced rituximab-induced NK cell IFN-γ secretion as well as in vitro cytotoxicity on mantle cell lymphoma cells; however, BGB-3111 was at least ten times less effective than ibrutinib in preventing rituximab-induced ADCC, which is in line with its feeble ITK inhibition activity.
| Targets |
BTK
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|---|---|
| ln Vitro |
BGB-3111 is more selective for BTK vs. EGFR, FGR, FRK, HER2, HER4, ITK, JAK3, LCK, BLK, and TEC than ibrutinib in biochemical and cellular assays[1].
BGB-3111 potently inhibits cell proliferation in multiple MCL and DLBCL cell lines by blocking downstream PLC-γ2 signaling and inhibiting BTK autophosphorylation triggered by BCR aggregation[2]. |
| ln Vivo |
BGB-3111 exhibits better oral bioavailability than ibrutinib in preclinical animal studies, achieving higher exposure and more complete target inhibition in the tissues[1].
BGB-3111 treatment causes a dose-dependent BTK occupancy in mouse BTK occupancy assays, and it exhibits approximately three times the potency of ibrutinib in target organs, such as the spleen and PBMC[2]. BGB-3111 exhibits better efficacy than ibrutinib and induces dose-dependent anti-tumor effects in both the REC-1 MCL and ABC subtype DLBCL (TMD-8) xenograft models. According to a rat toxicity study, BGB-3111 is highly well tolerated, and even at doses of up to 250 mg/kg/day, the MTD is not reached[3]. |
| References |
| Molecular Formula |
C27H29N5O3
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|---|---|---|
| Molecular Weight |
471.56
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| Exact Mass |
471.23
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| Elemental Analysis |
C, 68.77; H, 6.20; N, 14.85; O, 10.18
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| CAS # |
1691249-45-2
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| Related CAS # |
(±)-Zanubrutinib;1633350-06-7;(R)-Zanubrutinib;1691249-44-1;Zanubrutinib-d5
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| Appearance |
Solid powder
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| SMILES |
C=CC(=O)N1CCC(CC1)[C@@H]2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N
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| InChi Key |
RNOAOAWBMHREKO-QFIPXVFZSA-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)/t22-/m0/s1
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| Chemical Name |
(7S)-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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| 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 |
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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) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05356858 | Recruiting | Drug: zanubrutinib | Neuromyelitis Optica | Xuanwu Hospital, Beijing | May 7, 2022 | Phase 2 |
| NCT05199909 | Recruiting | Drug: zanubrutinib | Treatment Thrombocytopenia |
Zhang Lei, MD | January 25, 2022 | Phase 2 |
| NCT05320575 | Recruiting | Drug: Zanubrutinib | HLH | Beijing Friendship Hospital | January 26, 2021 | Phase 3 |
| NCT06029309 | Not yet recruiting | Drug: Zanubrutinib Drug: Tafasitamab |
Mantle Cell Lymphoma | Alvaro Alencar, MD | December 2023 | Phase 1 Phase 2 |
| NCT04172246 | Active Recruiting |
Drug: Zanubrutinib | Mature B-cell Malignancies | BeiGene | January 29, 2020 | Phase 1 Phase 2 |
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