规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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靶点 |
BTK
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体外研究 (In Vitro) |
在生化和细胞检测中,BGB-3111 对 BTK 与 EGFR、FGR、FRK、HER2、HER4、ITK、JAK3、LCK、BLK 和 TEC 的选择性比依鲁替尼更高[1]。
BGB-3111 有效抑制细胞通过阻断下游 PLC-γ2 信号传导并抑制 BCR 聚集触发的 BTK 自磷酸化来抑制多种 MCL 和 DLBCL 细胞系的增殖 [2]。 |
体内研究 (In Vivo) |
在临床前动物研究中,BGB-3111 表现出比依鲁替尼更好的口服生物利用度,在组织中实现了更高的暴露量和更完全的靶标抑制[1]。
BGB-3111 治疗导致小鼠 BTK 占用测定中出现剂量依赖性 BTK 占用,并且它在靶器官(如脾脏和 PBMC)中的效力约为依鲁替尼的三倍[2]。 BGB-3111 比依鲁替尼表现出更好的疗效,并在 REC-1 MCL 中诱导剂量依赖性抗肿瘤作用和 ABC 亚型 DLBCL (TMD-8) 异种移植模型。根据一项大鼠毒性研究,BGB-3111 具有高度良好的耐受性,即使剂量高达 250 mg/kg/天,也未达到 MTD[3]。 |
参考文献 |
分子式 |
C27H29N5O3
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分子量 |
471.56
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精确质量 |
471.23
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元素分析 |
C, 68.77; H, 6.20; N, 14.85; O, 10.18
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CAS号 |
1691249-45-2
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相关CAS号 |
(±)-Zanubrutinib;1633350-06-7;(R)-Zanubrutinib;1691249-44-1;Zanubrutinib-d5
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外观&性状 |
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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化学名 |
(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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别名 |
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
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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溶解度 (体外) |
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溶解度 (体内) |
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. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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 |
Aberrant activation of Bruton’s tyrosine kinase (BTK) plays an important role in pathogenesis of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of hematological malignancies. J Med Chem . 2019 Sep 12;62(17):7923-7940. td> |