货号:A730879 同义名: 伯舒替尼 (SKI-606) / SKI-606
Bosutinib is an inhibitor of Src and Abl with IC50 of 1.2 nM and 1 nM.
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产品名称 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
MNS |
+
Src, IC50: 29.3 μM |
p97,Syk | 98% | ||||||||||||||||
Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
PP121 |
++
Src, IC50: 14 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
Quercetin | ✔ | Sirtuin,PKC | 97% | ||||||||||||||||
Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
Repotrectinib |
+++
Src, IC50: 5.3 nM |
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。 |
靶点 |
|
描述 | Bosutinib is an orally active inhibitor of Src/Abl tyrosine kinases, with IC50 values of 1.2 nM and 1 nM, respectively[1]. Bosutinib is an active inhibitor of Bcr-Abl in various chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
23132-87 | Growth Inhibition Assay | IC50=15.8495 μM | SANGER | ||
5637 | Growth Inhibition Assay | IC50=1.13803 μM | SANGER | ||
647-V | Growth Inhibition Assay | IC50=29.7003 μM | SANGER | ||
697 | Growth Inhibition Assay | IC50=0.45633 μM | SANGER | ||
Animal study | Bosutinib, administered via oral gavage at a dose of 75 mg/kg twice daily, or 150 mg/kg once daily, is active against human KU812 xenografts in nude mice. Bosutinib, at 150 mg/kg once daily for 5 days a week, is effective against both wild-type Bcr-Abl and mutant Ba/F3 xenografts[2]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02551718 | Acute Leukemia of Ambiguous Li... 展开 >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia 收起 << | Not Applicable | Recruiting | - | United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker 206-616-1589 pbecker@u.washington.edu Principal Investigator: Pamela S. Becker 收起 << |
NCT03610971 | Chronic Phase Chronic Myeloid ... 展开 >>Leukemia Chronic Myeloid Leukemia, Chronic Phase 收起 << | Phase 2 | Not yet recruiting | January 2022 | United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute Not yet recruiting Tampa, Florida, United States, 33612 Contact: Anthony McLaughlin 813-745-5941 anthony.mclaughlin@moffitt.org Contact: Kendra Sweet, M.D. 813-745-8986 kendra.sweet@moffitt.org Principal Investigator: Kendra Sweet, M.D. 收起 << |
NCT03746054 | Chronic Myeloid Leukemia (CML) | Phase 3 | Not yet recruiting | March 2023 | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.89mL 0.38mL 0.19mL |
9.43mL 1.89mL 0.94mL |
18.85mL 3.77mL 1.89mL |
CAS号 | 380843-75-4 |
分子式 | C26H29Cl2N5O3 |
分子量 | 530.45 |
别名 | 伯舒替尼 (SKI-606) ;SKI-606 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 45 mg/mL(84.83 mM),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 |
动物实验配方 |
IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |