中文名 | 硫酸长春新碱 |
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英文名 | Vincristine Sulfate |
中文别名 |
替莫唑胺
硫酸醛基长春碱 长春新碱硫酸盐 |
英文别名 |
(3aR,4R,5S,5aR,10bR,13aR)-4-(acétyloxy)-3a-éthyl-9-[(13S,15S,17S)-17-éthyl-17-hydroxy-13-(méthoxycarbonyl)-1,11-diazatétracyclo[13.3.1.0.0]nonadéca-4(12),5,7,9-tétraén-13-yl]-6-formyl-5-hydroxy-8-méthoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate de méthyle sulfate (salt)
oncovin VCR Methyl-(3aR,4R,5S,5aR,10bR,13aR)-4-(acetyloxy)-3a-ethyl-9-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0.0]nonadeca-4(12),5,7,9-tetraen-13-yl]-6-form Vincrisul (2'b)-22-oxovincaleukoblastine sulfate (1:1) NovopharM V5 PEPTIDE kyocristine (2'β)-22-Oxovincaleukoblastine sulfate (1:1) 22-Oxovincaleukoblastine Sulfate (1:1) (salt) 22-oxovincaleukoblastine sulfate Vincristine sulfate salt onkovin MFCD00084729 methyl (3aR,4R,5S,5aR,10bR,13aR)-4-(acetyloxy)-3a-ethyl-9-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0.0]nonadeca-4(12),5,7,9-tetraen-13-yl]-6-formyl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate sulfate (salt) vincaleukoblastine, 22-oxo-, (2'b)-, sulfate (1:1) yl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate sulfate (salt) vincristin methyl (3aR,4R,5S,5aR,10bR,13aR)-4-(acetyloxy)-3a-ethyl-9-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0.0]nonadeca-4(12),5,7,9-tetraen-13-yl]-6-form Vincristine sulfate yl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazol-5-carboxylatsulfat(salt) Vincaleukoblastine, 22-oxo-, (2'β)-, sulfate (1:1) Methyl-(3aR,4R,5S,5aR,10bR,13aR)-4-(acetyloxy)-3a-ethyl-9-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0.0]nonadeca-4(12),5,7,9-tetraen-13-yl]-6-formyl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazol-5-carboxylatsulfat(salt) EINECS 218-190-0 (3aR,4R,5S,5aR,10bR,13aR)-4-(acétyloxy)-3a-éthyl-9-[(13S,15S,17S)-17-éthyl-17-hydroxy-13-(méthoxycarbonyl)-1,11-diazatétracyclo[13.3.1.0.0]nonadéca-4(12),5,7,9-tétraén-13-yl]-6-formyl-5-hy Vincristine (sulfate) Vincristine vincaleukoblastine, 22-oxo-, (3β,4'β)-, sulfate (1:1) 22-Oxovincaleukoblastine sulfate salt,Leurocristine sulfate salt,VCR droxy-8-méthoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate de méthyle sulfate (salt) |
描述 | Vincristine sulfate是一种抗肿瘤长春花生物碱,抑制有丝分裂纺锤体中的 microtubule 形成,导致中期阶段的分裂细胞停滞。 它与 microtubule 结合的 Ki 为85 nM。 |
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相关类别 | |
体外研究 | 长春新碱抑制稳态微管组装末端微管蛋白二聚体的净添加,Ki为85 nM [1]。长春新碱稳定心轴装置,导致染色体不能分离,导致中期停滞和低浓度的有丝分裂抑制。在较高浓度下,长春新碱可能会破坏并诱导微管的完全解聚[2]。长春新碱诱导肿瘤细胞凋亡,抑制SH-SY5Y细胞增殖,IC50为0.1μM。长春新碱诱导有丝分裂停滞并促进caspase-3和-9和cyclin B的表达,同时降低cyclin D的表达[3]。长春新碱诱导的神经毒性是由于干扰微管功能引起的,导致轴突运输受阻,从而导致轴突变性[4]。 |
体内研究 | 长春新碱(3mg/kg,ip)诱导平均生长延迟> 120和> 52天,并且重新填充0.06%和5%的组分,分别在携带双侧皮下异种移植物Rh12或Rh18的小鼠中给药[5]。 |
细胞实验 | 将细胞以约5×10 4个细胞/ mL的浓度接种在35mm板中的2mL培养基中,并在37℃,5%CO 2和95%空气的气氛中生长24小时。然后用缺乏或含有4nM药物的新鲜培养基替换培养基,并继续增殖3天。在用胰蛋白酶和EDTA分离细胞后,每天在库尔特计数器中进行细胞计数。 |
参考文献 |
[2]. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87. |
沸点 | 273-281 °C |
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熔点 | 300 °C |
分子式 | C46H58N4O14S |
分子量 | 923.036 |
精确质量 | 922.367004 |
PSA | 254.15000 |
LogP | 4.52220 |
外观性状 | 白色结晶粉末 |
储存条件 | 充氩气密封于4℃干燥避光保存。 |
水溶解性 | >=1 G/100 ML AT 24 ºC |
计算化学 | 1、 疏水参数计算参考值(XlogP): 2、 氢键供体数量:5 3、 氢键受体数量:16 4、 可旋转化学键数量:10 5、 互变异构体数量: 6、 拓扑分子极性表面积(TPSA):246 7、 重原子数量:65 8、 表面电荷:0 9、 复杂度:1830 10、同位素原子数量:0 11、确定原子立构中心数量:9 12、不确定原子立构中心数量:0 13、确定化学键立构中心数量:0 14、不确定化学键立构中心数量:0 15、共价键单元数量:2 |
更多 | 1. 性状:晶体状粉末,有恶臭气味。 2. 密度(g/mL,25/4℃): 未确定 3. 相对蒸汽密度(g/mL,空气=1):未确定 4. 熔点(ºC):300 ºC 5. 沸点(ºC,常压):273-281 ºC 6. 沸点(ºC,13mmHg):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 溶解性: >=1 g/100 mL at 24 ºC :。 |
Synonym:Leurocristine sulfate (1:1 Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
Risk Phrases: 23/24/25 Section 3 - HAZARDS IDENTIFICATION EMERGENCY OVERVIEW
Toxic by inhalation, in contact with skin and if swallowed.Hygroscopic (absorbs moisture from the air).Light sensitive. Potential Health Effects Eye: May cause eye irritation. Skin: May cause skin irritation. May be harmful if absorbed through the skin. Ingestion: May cause irritation of the digestive tract. May cause gastrointestinal irritation with nausea, vomiting and diarrhea. May cause liver and kidney damage. May cause bone marrow depression. Inhalation: May cause respiratory tract irritation. May cause effects similar to those described for ingestion. Chronic: Chronic exposure may cause reproductive disorders and teratogenic effects. Section 4 - FIRST AID MEASURES Eyes: Immediately flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid immediately. Skin: Get medical aid immediately. Immediately 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 immediately. Do NOT induce vomiting. If conscious and alert, rinse mouth and drink 2-4 cupfuls of milk or water. Inhalation: Get medical aid immediately. Remove from exposure and move to fresh air immediately. Do not use mouth-to-mouth resuscitation if victim ingested or inhaled the substance; induce artificial respiration with the aid of a pocket mask equipped with a one-way valve or other proper respiratory medical device. Notes to Physician: Treat symptomatically and supportively. 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. Extinguishing Media: Use carbon dioxide, dry chemical powder or water spray. Section 6 - ACCIDENTAL RELEASE MEASURES General Information: Use proper personal protective equipment as indicated in Section 8. Spills/Leaks: Wash area with soap and water. Clean up spills immediately, observing precautions in the Protective Equipment section. Sweep up, then place into a suitable container for disposal. Avoid generating dusty conditions. Provide ventilation. Section 7 - HANDLING and STORAGE Handling: Wash thoroughly after handling. Use with adequate ventilation. Do not get in eyes, on skin, or on clothing. Keep container tightly closed. Store protected from light. Use only in a chemical fume hood. Do not breathe dust or fumes. Storage: Store in a tightly closed container. Keep refrigerated. (Store below 4C/39F.) Store protected from moisture. Store protected from light. Store in a cool, dry area away from incompatible substances. 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# 2068-78-2: 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: white to pale yellow Odor: none reported pH: Not available. Vapor Pressure: Not available. Viscosity: Not available. Boiling Point: Not available. Freezing/Melting Point: > 300 deg C Autoignition Temperature: Not applicable. Flash Point: Not applicable. Explosion Limits, lower: Not available. Explosion Limits, upper: Not available. Decomposition Temperature: Not available. Solubility in water: soluble Specific Gravity/Density: Not available. Molecular Formula: C46H58N4O14S Molecular Weight: 923.03 Section 10 - STABILITY AND REACTIVITY Chemical Stability: Stable under normal temperatures and pressures. Light sensitive. Conditions to Avoid: Incompatible materials, excess heat, exposure to moist air or water, excess light. Incompatibilities with Other Materials: Strong oxidizing agents, heat, moisture, heavy metal salts, direct light. Hazardous Decomposition Products: Carbon monoxide, oxides of nitrogen, oxides of sulfur, irritating and toxic fumes and gases, carbon dioxide. Hazardous Polymerization: Will not occur. Section 11 - TOXICOLOGICAL INFORMATION RTECS#: CAS# 2068-78-2: OH6340000 LD50/LC50: Not available. Carcinogenicity: Vincristine sulfate - Not listed by ACGIH, IARC, or NTP. Other: See actual entry in RTECS for complete information. Section 12 - ECOLOGICAL INFORMATION Other No information available. Section 13 - DISPOSAL CONSIDERATIONS Dispose of in a manner consistent with federal, state, and local regulations. Section 14 - TRANSPORT INFORMATION IATA Shipping Name: TOXIC SOLID, ORGANIC, N.O.S.* Hazard Class: 6.1 UN Number: 2811 Packing Group: II IMO Shipping Name: TOXIC SOLID, ORGANIC, N.O.S. Hazard Class: 6.1 UN Number: 2811 Packing Group: II RID/ADR Shipping Name: TOXIC SOLID, ORGANIC, N.O.S. Hazard Class: 6.1 UN Number: 2811 Packing group: II Section 15 - REGULATORY INFORMATION European/International Regulations European Labeling in Accordance with EC Directives Hazard Symbols: T Risk Phrases: R 23/24/25 Toxic by inhalation, in contact with skin and if swallowed. Safety Phrases: S 24/25 Avoid contact with skin and eyes. 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# 2068-78-2: No information available. Canada None of the chemicals in this product are listed on the DSL/NDSL list. CAS# 2068-78-2 is not listed on Canada's Ingredient Disclosure List. US FEDERAL TSCA CAS# 2068-78-2 is not listed on the TSCA inventory. It is for research and development use only. SECTION 16 - ADDITIONAL INFORMATION N/A |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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符号 |
GHS06, GHS08 |
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信号词 | Danger |
危害声明 | H300-H341-H361fd |
警示性声明 | Missing Phrase - N15.00950417-P280 |
个人防护装备 | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
危害码 (欧洲) | T:Toxic |
风险声明 (欧洲) | R36/37/38;R61 |
安全声明 (欧洲) | 22-24/25-53-45-37/39-26-36/37/39 |
危险品运输编码 | UN 2811 6.1/PG 2 |
WGK德国 | 3 |
RTECS号 | OH6340000 |
包装等级 | II |
危险类别 | 6.1(a) |
海关编码 | 2942000000 |
上游产品 0 | |
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下游产品 1 | |
海关编码 | 2942000000 |
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