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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Bosutinib (SKI-606), 酪氨酸蛋白激酶 Lyn 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Bosutinib (SKI-606) is a potent c-Abl, Bcr-Abl, and Src-Abl kinase inhibitor, shown to effectively interfere with the progress of chronic myelogenous leukemia (CML). In a competitive study with Imatinib, Bosutinib was shown to inhibit Bcr-Abl kinase activity in CD34+ CML cells more potently than Imatinib. Activity of Src-Abl has been implicated in the development of other non-CML malignancies, and Bosutinib has demonstrated in studies to suppress breast cancer growth and migration.A c-Abl, Src-Abl, and Bcr-Abl inhibitor
Information
Bosutinib (SKI-606) is a novel, dualSrc/Ablinhibitor withIC50of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity ofPI3K/AKT/mTOR,MAPK/ERKandJAK/STAT3signaling pathways by blocking the phosphorylation lev
In vitro
Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin.
In vivo
Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts.
Cell Data
cell lines：Gli-Luc/MEF cells
Concentrations：Dissolved in DMSO, final concentrations ~1 μM
Incubation Time：72 hours
Powder Purity:≥98%
规格
别名
博舒替尼（SKI-606）
英文别名
4-(2,4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Bosutinib (SKI-606)
生化机理
博舒替尼（SKI-606）是一种新型 Src/Abl 双重抑制剂，在无细胞实验中的 IC50 分别为 1.2 nM 和 1 nM。博舒替尼还能通过阻断 p-ERK、p-S6 和 p-STAT3 的磷酸化水平，有效降低 PI3K/AKT/mTOR、MAPK/ERK 和 JAK/STAT3 信号通路的活性。博苏替尼能促进自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
酪氨酸蛋白激酶 Lyn 抑制剂
名称和识别符
EC号
700-455-1
分子类型
小分子
Isomeric SMILES
CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC
分子量
530.45
Reaxy-Rn
9100307
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9100307&ln=
技术文档
高级数据
产品属性
| ALogP | 5.4 |
|---|
关联靶点（人）
CTH
Tchem
胱硫醚γ-裂解酶(Cystathionine gamma-lyase)
(0 活性数据)
EPHA2
Tclin
肝素 A 型受体 2(Ephrin type-A receptor 2)
(1 活性数据)
EPHA4
Tchem
肝素 A 型受体 4(Ephrin type-A receptor 4)
(1 活性数据)
EPHA8
Tchem
肝素 A 型受体 8(Ephrin type-A receptor 8)
(1 活性数据)
EPHB4
Tchem
肝素 B 型受体 4(Ephrin type-B receptor 4)
(2 活性数据)
ERBB4
Tclin
受体酪氨酸蛋白激酶 erbB-4(Receptor tyrosine-protein kinase erbB-4)
(1 活性数据)
EPHA5
Tchem
肝素 A 型受体 5(Ephrin type-A receptor 5)
(1 活性数据)
ERBB3
Tclin
受体酪氨酸蛋白激酶 erbB-3(Receptor tyrosine-protein kinase erbB-3)
(1 活性数据)
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(4 活性数据)
EPHA3
Tchem
肝素 A 型受体 3(Ephrin type-A receptor 3)
(1 活性数据)
SRC
Tclin
原癌基因酪氨酸蛋白激酶Src(Proto-oncogene tyrosine-protein kinase Src)
(28 活性数据)
STK10
Tchem
丝氨酸/苏氨酸蛋白激酶10(Serine/threonine-protein kinase 10)
(2 活性数据)
STK24
Tchem
丝氨酸/苏氨酸蛋白激酶24(Serine/threonine-protein kinase 24)
(3 活性数据)
STK35
Tchem
丝氨酸/苏氨酸蛋白激酶 35(Serine/threonine-protein kinase 35)
(1 活性数据)
STK4
Tchem
丝氨酸/苏氨酸蛋白激酶 4(Serine/threonine-protein kinase 4)
(1 活性数据)
TXK
Tchem
酪氨酸蛋白激酶TXK(Tyrosine-protein kinase TXK)
(1 活性数据)
YES1
Tclin
酪氨酸蛋白激酶 是(Tyrosine-protein kinase Yes)
(2 活性数据)
FRK
Tchem
酪氨酸蛋白激酶 FRK(Tyrosine-protein kinase FRK)
(4 活性数据)
FYN
Tclin
酪氨酸蛋白激酶 Fyn(Tyrosine-protein kinase Fyn)
(3 活性数据)
GAK
Tchem
细胞周期蛋白G相关激酶(Cyclin-G-associated kinase)
(3 活性数据)
FGR
Tchem
酪氨酸蛋白激酶Fgr(Tyrosine-protein kinase Fgr)
(2 活性数据)
CAMK1D
Tchem
钙/钙调蛋白依赖性蛋白激酶 1D 型(Calcium/calmodulin-dependent protein kinase type 1D)
(1 活性数据)
SIK1
Tchem
丝氨酸/苏氨酸蛋白激酶 SIK1(Serine/threonine-protein kinase SIK1)
(1 活性数据)
SIK2
Tchem
丝氨酸/苏氨酸蛋白激酶SIK2(Serine/threonine-protein kinase SIK2)
(2 活性数据)
TNIK
Tchem
TRAF2 与 NCK 相互作用蛋白激酶(TRAF2 and NCK-interacting protein kinase)
(1 活性数据)
SIK3
Tchem
丝氨酸/苏氨酸蛋白激酶 SIK3(Serine/threonine-protein kinase SIK3)
(1 活性数据)
SLK
Tchem
STE20 类丝氨酸/苏氨酸蛋白激酶(STE20-like serine/threonine-protein kinase)
(1 活性数据)
PKMYT1
Tchem
膜相关酪氨酸和苏氨酸特异性 cdc2 抑制激酶(Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase)
(2 活性数据)
MINK1
Tchem
畸形类激酶1(Misshapen-like kinase 1)
(2 活性数据)
MAP2K2
Tclin
双特异性丝裂原活化蛋白激酶激酶 2(Dual specificity mitogen-activated protein kinase kinase 2)
(1 活性数据)
MAP4K2
Tchem
丝裂原活化蛋白激酶激酶激酶2(Mitogen-activated protein kinase kinase kinase kinase 2)
(2 活性数据)
LCK
Tclin
酪氨酸蛋白激酶Lck(Tyrosine-protein kinase Lck)
(2 活性数据)
MAP4K3
Tchem
丝裂原活化蛋白激酶激酶激酶 3(Mitogen-activated protein kinase kinase kinase kinase 3)
(2 活性数据)
MAP4K4
Tchem
丝裂原活化蛋白激酶激酶激酶 4(Mitogen-activated protein kinase kinase kinase kinase 4)
(1 活性数据)
MAP4K5
Tchem
丝裂原活化蛋白激酶激酶激酶 5(Mitogen-activated protein kinase kinase kinase kinase 5)
(4 活性数据)
LYN
Tclin
酪氨酸蛋白激酶 Lyn(Tyrosine-protein kinase Lyn)
(4 活性数据)
BTK
Tclin
酪氨酸蛋白激酶 BTK(Tyrosine-protein kinase BTK)
(3 活性数据)
BMX
Tchem
细胞质酪氨酸蛋白激酶 BMX(Cytoplasmic tyrosine-protein kinase BMX)
(2 活性数据)
BCR
Tclin
断点簇区域蛋白质(Breakpoint cluster region protein)
(1 活性数据)
BLK
Tchem
酪氨酸蛋白激酶 Blk(Tyrosine-protein kinase Blk)
(1 活性数据)
TNK2
Tclin
激活 CDC42 激酶 1(Activated CDC42 kinase 1)
(4 活性数据)
ABL2
Tchem
酪氨酸蛋白激酶 ABL2(Tyrosine-protein kinase ABL2)
(3 活性数据)
ABL1
Tclin
酪氨酸蛋白激酶ABL1(Tyrosine-protein kinase ABL1)
(23 活性数据)
HCK
Tclin
酪氨酸蛋白激酶HCK(Tyrosine-protein kinase HCK)
(3 活性数据)
NTRK2
Tclin
BDNF/NT-3 生长因子受体(BDNF/NT-3 growth factors receptor)
(1 活性数据)
NTRK1
Tclin
高亲和力神经生长因子受体(High affinity nerve growth factor receptor)
(1 活性数据)
CAMK2G
Tchem
钙/钙调蛋白依赖性蛋白激酶 II 型亚基γ(Calcium/calmodulin-dependent protein kinase type II subunit gamma)
(1 活性数据)
MAP2K1
Tclin
双特异性丝裂原活化蛋白激酶激酶 1(Dual specificity mitogen-activated protein kinase kinase 1)
(2 活性数据)
MAP2K5
Tchem
双特异性丝裂原活化蛋白激酶激酶 5(Dual specificity mitogen-activated protein kinase kinase 5)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 47 mg/mL (199.05 mM); Water: 47 mg/mL (199.05 mM); Ethanol: 10 mg/mL (42.35 mM);
安全和危险性（GHS）
象形图
危险声明
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
WGK Germany
3
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214617 |
分析证书 | B407917 |
技术文档和文章
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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