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| 中文名 | 星形孢菌素 |
|---|---|
| 英文名 | staurosporine |
| 中文别名 | 星孢菌素 |
| 英文别名 |
Stauroporine
6,10-Epoxy-6H,16H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-16-one, 7,8,9,10,17,18-hexahydro-7-methoxy-6-methyl-8-(methylamino)-, (6S,7R,8R,10R)- (2S,3R,4R,6R)-3-Methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1.0.0.0.0.0]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one Staurosporine staurosphorine ANTIBIOTIC M 193 MFCD00077402 Antibiotic 230 antibiotic am 2282 ANTIBIOTIC AM-2282 AM-2282 STSP Staurosporin |
| 描述 | Staurosporine是一种有效,非选择性蛋白激酶抑制剂,抑制 PKC,PKA,c-Fgr,和 Phosphorylase kinase 的 IC50 分别为 6 nM,15 nM,2 nM,3 nM。 |
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| 相关类别 | |
| 靶点 |
PKC:6 nM (IC50) c-Fgr:2 nM (IC50) Phosphorylase kinase:3 nM (IC50) v-Src:6 nM (IC50) cdc2:9 nM (IC50) TPK-IIB/Syk:16 nM (IC50) Ca2+/CaM PK-I1:20 nM (IC50) MLCK:21 nM (IC50) IR:61 nM (IC50) EGF-R:100 nM (IC50) ERK-1:1500 nM (IC50) CSK:2000 nM (IC50) IGF-IR:6150 nM (IC50) CK2:19500 nM (IC50) CK1:163500 nM (IC50) S6 kinase (70 kDa):5 nM (IC50) PKA:15 nM (IC50) |
| 体外研究 | Staurosporine广泛用作具有广谱活性的蛋白激酶C(PKC)抑制剂,是从Streptomyces staurospores的培养液中分离的生物碱。 MC3T3E-1成骨细胞暴露于Staurosporine(100 nM)12 h,释放出与对照细胞释放相似的LDH(12.4±3.1％)(10.0±2.4％),表明裂解相对缺失死亡,发生在坏死。此外,用星形孢菌素(100nM)处理导致形态学变化,细胞凋亡的特征：在Hoechst 33258染色后通过荧光显微镜观察到的亮蓝色荧光凝聚核,并且细胞体积减少[2]。 |
| 体内研究 | 星形孢菌素的抑制作用在肿瘤促进的Wk10左右具有统计学意义。尽管在实验的后几周中10ng的星形孢菌素没有获得统计学上显着的抑制,但是带有肿瘤的小鼠的百分比和每只小鼠的平均肿瘤数量的下降趋势是明显的。因此,Staurosporine稍微抑制了Teleocidin的肿瘤促进,即使在Staurosporine本身诱发肿瘤的剂量[3]。即使在病变后2周开始给药,Staurosponne(0.05和0.1 mg/kg腹膜内)减弱了水迷宫和被动回避任务的受损性能。此外,Staurosporine(0.1 mg/kg)部分逆转了由基底前脑损伤引起的额顶皮质中胆碱乙酰转移酶活性的降低。这些结果表明,Staurosporine通过逆转基底前脑损伤诱导的胆碱能神经元损伤减轻学习障碍[4]。 |
| 激酶实验 | 将MC3T3E-1细胞（2×10 6个细胞/组）用100nM星形孢菌素处理不同的时间段并在裂解缓冲液中裂解（EB缓冲液：1％Triton X-100,10mM Tris，pH 7.6,50mM NaCl， 1mg / mL抑肽酶，5mM EDTA，50mM NaF，0.1％2-巯基乙醇和100μM原钒酸钠）。将细胞裂解物在12000g，4℃下离心30分钟。收集可溶性级分并与抗JNK1抗体一起温育。在冰上孵育3小时后，将100μL10％福尔马林固定的金黄色葡萄球菌溶液加入到抗JNK1免疫沉淀物中，并进一步在冰上孵育1小时。用EB缓冲液和PAN缓冲液（10mM PIPES缓冲液，pH7.0,1％抑肽酶，100mM NaCl）洗涤吸收的免疫复合物两次。免疫复合物与2μgGST-c-Jun NT1-79蛋白作为底物在30μL含有2μM冷ATP，2 mM DTT，20 mMMgCl2,2μCi[γ33-P] -ATP的反应缓冲液中混合和20mM Tris-HCl，pH 7.5,30℃，20分钟。通过加入15μL3×SDS-PAGE样品缓冲液并在98℃下煮沸5分钟终止反应。蛋白质在12％SDS-PAGE上分离，并通过半干电转移系统转移到硝酸纤维素膜上。用兔抗JNK1抗体和辣根过氧化物酶缀合的抗兔抗体对膜进行免疫印迹，以显现通过增强的化学发光系统测量的信号。将凝胶在真空下干燥，通过放射自显影观察磷酸转移酶活性，并通过PhosphoImager分析仪定量[2]。 |
| 动物实验 | 小鼠[3]使用雌性CD-1小鼠。将10μL丙酮中的各种量的星形孢菌素施用于8周龄CD-1小鼠的耳朵。刺激程度表示为引起刺激的化合物的最小剂量。小鼠皮肤中HOC的诱导将0.1mL丙酮中的星形孢菌素施用于CD-1小鼠背部的皮肤，18小时后从皮肤获得粗酶提取物。 HDC活性表示为每1h孵育每mg蛋白质释放的CO 2 pmol。诱导小鼠皮肤中的ODC将0.2mL丙酮中的星形孢菌素施用于CD-1小鼠背部的皮肤。 4小时后，从表皮制备粗酶提取物，并测量其ODC活性。酶活性表示为每30分钟孵育每mg蛋白质的nmol CO2。大鼠[4]使用雄性Kbl Wistar大鼠（体重270至310g）。在给予星形孢菌素2周的组中，在BF损伤后2周开始水迷宫任务和星形孢菌素给药，并且在BFlesion后4周进行被动回避任务。在水迷宫训练和被动回避任务采集之前30mm，大鼠接受剂量为0.01,0.03,0.1和0.3mg / kg（ip，每组N = 10，持续2周）的Staurosporine。在给予星形孢菌素4周的组中，首先在BF损伤后2周给予药物。水迷宫任务在BF损伤后4周进行。被动回避任务在BF病变后6周进行。大鼠在训练前每天一次接受0.05,0.1和0.2 mg / kg（ip，N =每组10）的Staurosporine，持续2周，在水迷宫训练和被动回避任务获取试验后持续2周。将星形孢菌素悬浮在0.3％的羧甲基纤维素钠中。将载体以与星形孢菌素处理的动物相同的方案施用于未损伤的对照和损伤的对照。 |
| 参考文献 |
| 密度 | 1.6±0.1 g/cm3 |
|---|---|
| 沸点 | 677.5±55.0 °C at 760 mmHg |
| 熔点 | 270ºC |
| 分子式 | C28H26N4O3 |
| 分子量 | 466.531 |
| 闪点 | 363.6±31.5 °C |
| 精确质量 | 466.200500 |
| PSA | 69.45000 |
| LogP | 4.40 |
| 外观性状 | 灰白色粉末 |
| 蒸汽压 | 0.0±2.1 mmHg at 25°C |
| 折射率 | 1.810 |
| 储存条件 | 0-10°C;存放于惰性气体之中;避免空气,加热 |
| 分子结构 | 1、 摩尔折射率：128.82 2、 摩尔体积（m3/mol）：298.7 3、 等张比容（90.2K）：841.1 4、 表面张力（dyne/cm）：62.8 5、 极化率（10-24cm3）：51.06 |
| 计算化学 | 1、 疏水参数计算参考值（XlogP）：3.2 2、 氢键供体数量：2 3、 氢键受体数量：4 4、 可旋转化学键数量：2 5、 拓扑分子极性表面积（TPSA）：69.5 6、 重原子数量：35 7、 表面电荷：0 8、 复杂度：901 9、 同位素原子数量：0 10、 确定原子立构中心数量：4 11、 不确定原子立构中心数量：0 12、 确定化学键立构中心数量：0 13、 不确定化学键立构中心数量：0 14、 共价键单元数量：1 |
| 更多 | 1. 性状：。 2. 密度（g/mL,25/4℃）： 3. 相对蒸汽密度（g/mL,空气=1）：未确定 4. 熔点（ºC）： 5. 沸点（ºC,常压）： 6. 沸点（ºC,5.2kPa）：未确定 7. 折射率：未确定 8. 闪点（ºC）：未确定 9. 比旋光度（º）：未确定 10. 自燃点或引燃温度（ºC）：未确定 11. 蒸气压（kPa,25ºC）：未确定 12. 饱和蒸气压（kPa,60ºC）：未确定 13. 燃烧热（KJ/mol）：未确定 14. 临界温度（ºC）：未确定 15. 临界压力（KPa）：未确定 16. 油水（辛醇/水）分配系数的对数值：未确定 17. 爆炸上限（%,V/V）：未确定 18. 爆炸下限（%,V/V）：未确定 19. 溶解性：。 |
Synonym:Antibiotic AM-228 Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
Risk Phrases: 40 Section 3 - HAZARDS IDENTIFICATION EMERGENCY OVERVIEW
Limited evidence of a carcinogenic effect.Light sensitive.Moisture sensitive.The toxicological properties of this material have not been fully investigated. Potential Health Effects Eye: May cause eye irritation. Skin: May cause skin irritation. Ingestion: May cause irritation of the digestive tract. The toxicological properties of this substance have not been fully investigated. Inhalation: May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated. Chronic: No information found. Section 4 - FIRST AID MEASURES Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid. Skin: Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Wash clothing before reuse. Ingestion: Never give anything by mouth to an unconscious person. Get medical aid. Do NOT induce vomiting. If conscious and alert, rinse mouth and drink 2-4 cupfuls of milk or water. Wash mouth out with water. Inhalation: Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid. Notes to Physician: Section 5 - FIRE FIGHTING MEASURES General Information: As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. Non-combustible, substance itself does not burn but may decompose upon heating to produce irritating, corrosive and/or toxic fumes. Extinguishing Media: Substance is noncombustible; use agent most appropriate to extinguish surrounding fire. Do NOT get water inside containers. Use water spray, dry chemical, carbon dioxide, or appropriate foam. Section 6 - ACCIDENTAL RELEASE MEASURES General Information: Use proper personal protective equipment as indicated in Section 8. Spills/Leaks: Vacuum or sweep up material and place into a suitable disposal container. Clean up spills immediately, observing precautions in the Protective Equipment section. Avoid generating dusty conditions. Provide ventilation. Do not get water inside containers. Section 7 - HANDLING and STORAGE Handling: Wash thoroughly after handling. Use with adequate ventilation. Minimize dust generation and accumulation. Avoid contact with eyes, skin, and clothing. Keep container tightly closed. Avoid ingestion and inhalation. Store protected from light. Do not allow contact with water. Keep from contact with moist air and steam. Storage: Do not store in direct sunlight. Store in a tightly closed container. Store in a cool, dry, well-ventilated area away from incompatible substances. Keep refrigerated. (Store below 4C/39F.) Store protected from moisture. Store protected from light. Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION Engineering Controls: Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low. Exposure Limits CAS# 62996-74-1: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166. Skin: Wear appropriate protective gloves to prevent skin exposure. Clothing: Wear appropriate protective clothing to prevent skin exposure. Respirators: A respiratory protection program that meets OSHA's 29 CFR 1910.134 and ANSI Z88.2 requirements or European Standard EN 149 must be followed whenever workplace conditions warrant respirator use. Section 9 - PHYSICAL AND CHEMICAL PROPERTIES Physical State: Powder Color: off-white Odor: none reported pH: Not available. Vapor Pressure: Not available. Viscosity: Not available. Boiling Point: Not available. Freezing/Melting Point: 270 deg C Autoignition Temperature: Not applicable. Flash Point: Not applicable. Explosion Limits, lower: Not available. Explosion Limits, upper: Not available. Decomposition Temperature: Solubility in water: Specific Gravity/Density: Molecular Formula: C28H26N4O3 Molecular Weight: 466.207 Section 10 - STABILITY AND REACTIVITY Chemical Stability: Stable at room temperature in closed containers under normal storage and handling conditions. Conditions to Avoid: Incompatible materials, light, moisture, excess heat, exposure to moist air or water. Incompatibilities with Other Materials: Moisture, strong oxidizing agents. Hazardous Decomposition Products: Hydrogen chloride, nitrogen oxides, carbon monoxide, irritating and toxic fumes and gases, carbon dioxide. Hazardous Polymerization: Will not occur. Section 11 - TOXICOLOGICAL INFORMATION RTECS#: CAS# 62996-74-1: KC6550000 LD50/LC50: Not available. Carcinogenicity: Staurosporine - Not listed by ACGIH, IARC, or NTP. Other: See actual entry in RTECS for complete information. Section 12 - ECOLOGICAL INFORMATION Section 13 - DISPOSAL CONSIDERATIONS Dispose of in a manner consistent with federal, state, and local regulations. Section 14 - TRANSPORT INFORMATION IATA No information available. IMO No information available. RID/ADR No information available. Section 15 - REGULATORY INFORMATION European/International Regulations European Labeling in Accordance with EC Directives Hazard Symbols: XN Risk Phrases: R 40 Limited evidence of a carcinogenic effect. Safety Phrases: S 28A After contact with skin, wash immediately with plenty of water. S 36/37 Wear suitable protective clothing and gloves. S 37 Wear suitable gloves. S 45 In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible). WGK (Water Danger/Protection) CAS# 62996-74-1: No information available. Canada None of the chemicals in this product are listed on the DSL/NDSL list. CAS# 62996-74-1 is not listed on Canada's Ingredient Disclosure List. US FEDERAL TSCA CAS# 62996-74-1 is not listed on the TSCA inventory. It is for research and development use only. SECTION 16 - ADDITIONAL INFORMATION N/A |
| 符号 |
GHS08 |
|---|---|
| 信号词 | Danger |
| 危害声明 | H340-H350 |
| 警示性声明 | P201-P280-P308 + P313 |
| 个人防护装备 | Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges |
| 危害码 (欧洲) | Xn;T;Xi |
| 风险声明 (欧洲) | R40 |
| 安全声明 (欧洲) | S53-S36-S37 |
| 危险品运输编码 | UN 2811 6.1 / PGII |
| WGK德国 | 2 |
| RTECS号 | KC6550000 |
| 海关编码 | 29419090 |
| 上游产品 2 | |
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| 下游产品 0 | |
