质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
tan
溶解性
DMSO: 6 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
[n]21c3c4[n](c7c(c4c8c(c3c9c2cccc9)CNC8=O)cccc7)[C@@H]5O[C@]1([C@@]([C@@H]5N(C)C(=O)c6ccccc6)(OC)C)C
InChI
1S/C35H30N4O4/c1-34(42-4)30(37(3)32(41)19-12-6-5-7-13-19)33-38-23-16-10-8-14-20(23)26-27-22(18-36-31(27)40)25-21-15-9-11-17-24(21)39(29(25)28(26)38)35(34,2)43-33/h5-17,30,33H,18H2,1-4H3,(H,36,40)/t30-,33-,34-,35+/m1/s1
InChI key
IIQIEMHSDLLZQA-QZPVEUDVSA-N
一般描述
A cell-permeable Staurosporine (Cat. No. 569397) derivative that displays antitumor properties. Acts as a broad-spectrum, reversible, and ATP-competitive inhibitor of PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR (IC50 = 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM, respectively). At higher concentrations, also inhibits Ins-R and IGF-1R (IC50 = 10 µM). Shown to potently inhibit the proliferation of Ba/F3 cells expressing constitutively active Flt3 (IC50<10 nM).
生化/生理作用
Cell permeable: yes
Primary Target
PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR
PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR
Product competes with ATP.
Reversible: yes
Target IC50: 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM against primary targets in the order listed
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Weisberg, E., et al. 2002. Cancer Cell1, 433.
Fabbro, D., et al. 2000. Anticancer Drug Des.15, 17.
Meyer, T., et al. 1999. Int. J. Cancer81, 669.
Meyer, T., et al. 1989. Int. J. Cancer43, 851.
Fabbro, D., et al. 2000. Anticancer Drug Des.15, 17.
Meyer, T., et al. 1999. Int. J. Cancer81, 669.
Meyer, T., et al. 1989. Int. J. Cancer43, 851.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
警示用语:
Danger
危险声明
危险分类
Repr. 1B
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Bei Wang et al.
Redox biology, 65, 102825-102825 (2023-08-03)
Chemotherapeutic agents, such as doxorubicin (DOX), may cause cardiomyopathy, even life-threatening arrhythmias in cancer patients. Ferroptosis-an iron-dependent oxidative form of programmed necrosis, plays a pivotal role in DOX-induced cardiomyopathy (DIC). Prostaglandins (PGs) are bioactive signaling molecules that profoundly modulate cardiac
Oxana V Denisova et al.
Scientific reports, 12(1), 13796-13796 (2022-08-14)
Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially overcome kinase inhibitor resistance. However, in most cases
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