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卡铂

卡铂用途

Carboplatin (NSC 241240) 是一种 DNA 合成抑制剂,其与 DNA 结合,抑制复制和转录并诱导细胞死亡。Carboplatin (NSC 241240) 是顺铂的衍生物,是一种有效的抗癌剂。

卡铂名称

[ CAS 号 ]:
41575-94-4

[ 中文名 ]:
卡铂

[ 英文名 ]:
Carboplatin

[中文别名 ]:

[英文别名 ]:

cbdca
MFCD00070464
JM-8
PARAPLATIN
PARAPLATIN(R)
CARBONPLATIN
CARBOPLATINUM
EINECS 255-446-0
Carboplatin

卡铂生物活性

[ 描述 ]:

Carboplatin (NSC 241240) 是一种 DNA 合成抑制剂,其与 DNA 结合,抑制复制和转录并诱导细胞死亡。Carboplatin (NSC 241240) 是顺铂的衍生物,是一种有效的抗癌剂。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

研究领域 >> 癌症

[ 靶点 ]

DNA Alkylator[1]

[体外研究]

卡铂是一种抗肿瘤剂,在亲核试剂和人乳腺癌MCF-7细胞胞浆提取物存在下具有增强的DNA结合活性[1]。与17-AAG相比,卡铂对人卵巢细胞如A2780,SKOV3,IGROV1和HX62的细胞毒性较低,IC50分别为6.177,12.442,2.233和116.068μM。此外,卡铂不影响HSP90或改变17-AAG的活性以抑制HSP90 [2]。卡铂降低了Brca1(IC50,3.4μM)和Brca2细胞(IC50,1.9μM)的活力。卡铂(25μM)与ABT-888结合也在BRCA1细胞中显示出凋亡作用[3]。

[体内研究]

卡铂(60 mg/kg,ip)对肿瘤有轻微影响,但在携带A2780人卵巢癌异种移植物的小鼠中与17-AAG联合显着抑制肿瘤生长[2]。卡铂(25mg/kg,口服)与ABT-888联合可延迟Brca2异种移植物中的肿瘤生长[3]。

[细胞实验]

将指数生长的A2780细胞接种在96孔微量滴定板中。对于研究暴露于17-AAG或卡铂的序列的影响的实验，将细胞暴露于递增浓度的17-AAG或卡铂24小时。选择暴露于第一药剂24小时的时间段，使得A2780细胞暴露于第一药物至少一倍的倍增时间（18-24小时）。然后用无菌磷酸盐缓冲盐水洗涤细胞并补充培养基。此后，加入第二种药物（细胞在前24小时未暴露于其中）或培养基96小时。进行SRB测定。所有实验一式三份进行[2]。

[动物实验]

小鼠[2]通过在每个侧腹中注射4×10 6个细胞，将A2780人卵巢癌细胞系在雌性无胸腺NCr裸鼠（nu / nu）中作为皮下异种移植物生长。将具有相当于0.69mm 3的平均体积的确定肿瘤的小鼠随机分组（每组6只动物）用对照载体（43％乙醇，33％聚丙二醇和24％cremaphor用无菌水以1：7稀释）处理第1天-4,17-AAG（腹膜内80mg / kg，第1-4天），卡铂（60mg / kg IP第0天）或17-AAG（80mg / kg IP第1-4天）和卡铂（ 60mg / kg IP天0）。每周评估肿瘤生长三次，并根据验证的公式计算肿瘤体积：体积= 4.19×（a / 4 + b / 4）3，其中a是较长的b和较短的直径。然后将肿瘤体积表示为治疗开始时体积的比例（相对肿瘤体积）[2]。

[参考文献]

[1]. Natarajan G, et al. Increased DNA-binding activity of cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts: activation theory revisited. Biochem Pharmacol. 1999 Nov 15;58(10):1625-9.

[2]. Banerji U, et al. An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models. Cancer Chemother Pharmacol. 2008 Oct;62(5):769-78.

[3]. Clark CC, et al. Enhancement of synthetic lethality via combinations of ABT-888, a PARP inhibitor, and carboplatin in vitro and in vivo using BRCA1 and BRCA2 isogenic models. Mol Cancer Ther. 2012 Sep;11(9):1948-58.

[4]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116.

[相关活性小分子]

卡铂物理化学性质

[ 沸点 ]:
366.4ºCat 760 mmHg

[ 熔点 ]:
228-230ºC

[ 分子式 ]:
C₆H₁₂N₂O₄Pt

[ 分子量 ]:
371.254

[ 闪点 ]:
189.6ºC

[ 精确质量 ]:
371.044495

[ PSA ]:
59.08000

[ LogP ]:
0.81700

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
Store at RT

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
Sparingly soluble in water, very slightly soluble in acetone and in ethanol (96 per cent). | Soluble in water.

卡铂MSDS

详细MSDS(安全技术说明书)

卡铂毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TP2300000

CHEMICAL NAME :: Platinum, diammine(1,1-cyclobutanedicarboxylato(2-)-O,O')-, (SP-4-2)-

CAS REGISTRY NUMBER :: 41575-94-4

LAST UPDATED :: 199803

DATA ITEMS CITED :: 33

MOLECULAR FORMULA :: C6-H12-N2-O4-Pt

MOLECULAR WEIGHT :: 371.29

WISWESSER LINE NOTATION :: L4TJ AVQ AVQ &Z-PT-Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 343 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60900 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 118 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 89360 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 180 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >31200 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 158 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 70 mg/kg/2W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - changes in lung weight Endocrine - changes in spleen weight Blood - changes in platelet count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 140 mg/kg/26W-I

TOXIC EFFECTS :: Blood - normocytic anemia Blood - changes in bone marrow (not otherwise specified) Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 60 mg/kg/5D-I

TOXIC EFFECTS :: Gastrointestinal - alteration in gastric secretion Gastrointestinal - other changes Blood - hemorrhage

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 24 mg/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 24 mg/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: DNA damage

TYPE OF TEST :: DNA inhibition

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Morphological transformation

TEST SYSTEM :: Rodent - hamster Kidney

DOSE/DURATION :: 25 umol/L

REFERENCE :: EJCODS European Journal of Cancer and Clinical Oncology. (Pergamon Press, c/o Elsevier Science, 660 White Plains Rd., Tarrytown, NY 10591) V.17(7)- 25, 1981-89. For publisher information, see EJCAEL Volume(issue)/page/year: 25,27,1989 *** REVIEWS *** TOXICOLOGY REVIEW JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 65,315,1976

卡铂安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302 + H312 + H332-H317-H334-H340-H360

[ 警示性声明 ]:
P201-P261-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;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) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R46;R61;R20/21;R42/43

[ 安全声明 (欧洲) ]:
S53-S22-S26-S36/37/39-S45

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
TP2300000

[ 海关编码 ]:
2843900030

卡铂合成路线

详细合成路线

卡铂上下游产品

卡铂上游产品

卡铂下游产品

卡铂制备

氯铂酸钾和盐酸肼及碘化钾反应，得到顺碘氨铂，可用二甲基甲酰胺和乙醇的混合液重结晶来提纯。顺碘氨铂加入水中，缓缓滴加硫酸银，反应完毕。滤去不溶物，在滤液中缓缓加入1,1-环丁烷二羧酸钡，室温反应、静置、过滤、蒸干滤液。所得固体分别用水及乙醇洗涤。干燥后得卡铂。

卡铂海关

[ 海关编码 ]: 2843900030

卡铂文献

Mer590, a novel monoclonal antibody targeting MER receptor tyrosine kinase, decreases colony formation and increases chemosensitivity in non-small cell lung cancer.

Oncotarget 5(21) , 10434-45, (2014)

The successes of targeted therapeutics against EGFR and ALK in non-small cell lung cancer (NSCLC) have demonstrated the substantial survival gains made possible by precision therapy. However, the majo...

Graphene oxide - gelatin nanohybrids as functional tools for enhanced Carboplatin activity in neuroblastoma cells.

Pharm. Res. 32 , 2132-43, (2015)

Preparation of Nanographene oxide (NGO) - Gelatin hybrids for efficient treatment of Neuroblastoma.Nanohybrids were prepared via non-covalent interactions. Spectroscopic tools have been used to discri...

CD157 enhances malignant pleural mesothelioma aggressiveness and predicts poor clinical outcome.

Oncotarget 5(15) , 6191-205, (2014)

Malignant mesothelioma is a deadly tumor whose diagnosis and treatment remain very challenging. There is an urgent need to advance our understanding of mesothelioma biology and to identify new molecul...

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卡铂