Vecabrutinib是一种强效的 BTK 抑制剂,对 WT BTK 和 C481S BTK 的 IC50 分别为 4.6 nM 和 1.1 nM,同时还抑制 ITK 活性(IC50 = 24 nM)。
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产品名称 | BTK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
CGI-1746 |
+++
BTK, IC50: 1.9 nM |
99% (HPLC) | |||||||||||||||||
Spebrutinib |
++++
BTK, IC50: <0.5 nM |
98+% | |||||||||||||||||
Acalabrutinib |
++
BTK, IC50: 3nM |
98% | |||||||||||||||||
CNX-774 |
+++
BTK, IC50: <1 nM |
99%+ | |||||||||||||||||
Ibrutinib |
++++
BTK, IC50: 0.5 nM |
98% | |||||||||||||||||
ONO-4059 analog |
+
BTK, IC50: 23.9 nM |
98% | |||||||||||||||||
RN486 |
++
BTK, IC50: 4 nM |
99%+ | |||||||||||||||||
(Z)-LFM-A13 |
+
BTK, Ki: 1.4 μM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Bruton’s tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases and expressed in B cells, macrophages, and monocytes but not in T cells, plays a crucial role in signaling through the B cell receptor (BCR) and the Fcγ receptor (FcγR) in B cells and myeloid cells, respectively [1]. Vecabrutinib is a potent, noncovalent BTK and ITK (interleukin-2-inducible kinase) inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively. It inhibits WT and C481S BTK with IC50s of 2.9 nM and 4.4 nM, respectively. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%. Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours and is well tolerated with continuous drug levels. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03037645 | Chronic Lymphocytic Leukemia ... 展开 >> Small Lymphocytic Lymphoma Lymphoplasmacytoid Lymphoma Mantle-Cell Lymphoma Waldenstrom Macroglobulinemia Diffuse Large B Cell Lymphoma Follicular Lymphoma 收起 << | Phase 1 Phase 2 | Recruiting | June 30, 2021 | United States, California ... 展开 >> University of California Irvine Medical Center Recruiting Orange, California, United States, 92868-3201 Contact: General Contact 877-827-8839 ucstudy@uci.edu UC San Diego Moores Cancer Center Recruiting San Diego, California, United States, 92093 Contact: Barbara Ivers 858-822-6281 bivers@ucsd.edu United States, Florida Moffitt Cancer Center and Research Institute Recruiting Tampa, Florida, United States, 33612 Contact: Natalie Miller 813-745-2591 Natalie.Miller@moffitt.org United States, Massachusetts Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Conner Shaughnessy 617-582-8437 Conner_Shaughnessy@dfci.harvard.edu United States, New York Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Isaac Deonarine 646-888-1319 deonarii@mskcc.org Weill Cornell Medicine Recruiting New York, New York, United States, 10065 Contact: Jessica Harper 646-962-9414 jah2070@med.cornell.edu United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Chongjuan Wei 713-792-3530 cwei@mdanderson.org United States, Washington Swedish Cancer Institute Recruiting Seattle, Washington, United States, 98104 Contact: Ngan Trinh 206-215-2363 Ngan.Trinh@Swedish.org 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.89mL 0.38mL 0.19mL |
9.44mL 1.89mL 0.94mL |
18.87mL 3.77mL 1.89mL |
CAS号 | 1510829-06-7 |
分子式 | C22H24ClF4N7O2 |
分子量 | 529.918 |
别名 | SNS-062 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 120 mg/mL(226.45 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |