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靶点 |
DNA Alkylator/Crosslinker
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体外研究 (In Vitro) |
体外活性:顺铂是一种无机铂络合物,是一种化疗剂,也是多种细胞类型生长停滞和凋亡的有效诱导剂。它用于治疗多种癌症,包括睾丸癌、卵巢癌、宫颈癌、乳腺癌、膀胱癌、头颈癌、食道癌、肺癌、间皮瘤、脑肿瘤和神经母细胞瘤。 IV(静脉内)给药后,顺铂形成高反应性、带电荷的铂络合物,该络合物与 DNA 中富含 GC 的位点等亲核基团结合,诱导链内和链间 DNA 交联,以及 DNA-蛋白质交联。这会抑制 DNA 合成并导致细胞凋亡和细胞生长抑制。顺铂通过与 DNA 相互作用形成 DNA 加合物来诱导细胞毒性,从而激活多种信号转导途径,包括 Erk、p53、p73 和 MAPK,最终导致细胞凋亡的激活。顺铂 (30 mM) 处理 6 小时可诱导 HeLa 细胞中 Erk 明显激活,并在接下来的 14 小时内持续。顺铂还通过诱导肿瘤细胞死亡而显示出有效的抗肿瘤活性。顺铂表现出引起肾近端肾小管细胞 (RPTC) 凋亡的能力,导致细胞收缩、半胱天冬酶 3 活性增加 50 倍、磷脂酰丝氨酸外化增加 4 倍、染色质浓缩和 DNA 增加 5 倍和 15 倍分别为亚倍体。顺铂 (800 μM) 治疗 4 小时后会导致 RPTC 坏死的典型特征。细胞测定:L1210/0 细胞在补充有 15% 小牛血清和 Fungizone 的 McCoys 培养基 5a(改良)中于 37℃、5% CO2 潮湿气氛中维持指数悬浮培养。 L1210/0 细胞在顺铂 (7 μg/mL) 中于 37 ℃ 孵育 2 小时。为了测量生长抑制,将细胞离心,洗涤一次,以 30 × 103 至 50 × 103 细胞/mL 重悬于新鲜培养基中,并孵育 3 天。细胞数在库尔特计数器上测定。将等份细胞用等体积的 0.4% 台盼蓝稀释。活力记录为排除台盼蓝的细胞的百分比。将如上所述与顺铂一起孵育的细胞也稀释到 0.1% 琼脂中,并在对集落进行计数时使其生长 2 周。
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体内研究 (In Vivo) |
顺铂已被证明可有效抑制多种动物肿瘤模型中的肿瘤生长,包括头颈癌异种移植物、宫颈鳞状细胞癌异种移植物、睾丸癌异种移植物、卵巢癌异种移植物、乳腺癌异种移植物、结肠癌、异种移植肝母细胞瘤、等等。在第 1 天和第 7 天每周静脉注射顺铂 (5 mg/kg),可分别诱导浆液性异种移植物 Ov.Ri(C) 和 OVCAR-3 77.5% 和 85.1% 的肿瘤生长抑制 (GI)。
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动物实验 |
Mice: There are twenty mice per group, which are randomly assigned to three groups: Control, Cisplatin, and Cisplatin+HemoHIM. A subcutaneous femoral left region in mice is injected with B16F0 melanoma (5×105 cells/mouse) three days prior to the first Cisplatin injection. Three injections of 4 mg/kg body weight (B.W.) of cisplatin are administered intraperitoneally on days 0 through 14. Day 0 to Day 16 see daily intubations of the experimental group with HemoHIM at a final concentration of 100 mg/kgB.W., while the control group was given only water. Each group's mice undergo experiments on day 17 following their first Cisplatin injection in order to assess the tumors' size or weight. The tumor size is calculated as follows: tumor size=ab2/2, where a and b are the larger and smaller diameters, respectively.
Rats: Four groups of four or five male Sprague-Dawley rats, weighing 200 to 250 g apiece, are randomly assigned. First, a vehicle containing 5% carboxymethyl cellulose sodium solution (CMC-Na), 5 mL/kg body weight, p.o., was administered to the control group (Cap). The third group was injected with 5% CMC-Na for six consecutive days along with 5 mg/kg of Cisplatin in physiological saline solution intraperitoneally (i.p.). The second group received Cap (10 mg/kg/d, p.o.) in 5% CMC-Na (5 mL/kg). Six days straight after receiving an injection of 5 mg/kg of Cisplatin intraperitoneally (i.p.), the fourth group was given Cap (10 mg/kg/d, p.o.) in 5% CMC-Na. Every group receives a cap or vehicle twice a day. Data from our preliminary experiments are used to determine the chosen Cap concentration and the dose administration schedule without causing any intestinal damage in rats. |
参考文献 |
分子式 |
CL2H6N2PT
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分子量 |
300.05
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元素分析 |
Cl, 23.63; H, 2.02; N, 9.34; Pt, 65.02
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CAS号 |
15663-27-1
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外观&性状 |
Yellow solid powder
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SMILES |
Cl[Pt-2]([NH3+])([NH3+])Cl
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InChi Key |
LXZZYRPGZAFOLE-UHFFFAOYSA-L
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InChi Code |
InChI=1S/2ClH.2H3N.Pt/h2*1H;2*1H3;/q;;;;+2/p-2
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化学名 |
(SP-4-2)-diamminedichloroplatinum; platinum, diaminedichloro-, cis-
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别名 |
Cismaplat; Cisplatina; cisplatinous diamine dichloride; cisplatinum; cisplatinum II; cisplatinum II diamine dichloride; CDDP; DDP; cisDDP; cisdiamminedichloro platinum (II); cisdiamminedichloroplatinum; Cisdichloroammine Platinum (II); CPDD; Cysplatyna; DDP; PDD; Peyrones Chloride; Peyrones Salt; CACP; Platinoxan; platinum diamminodichloride. Trade names (US): Platinol; PlatinolAQ. Trade names (other countries): Abiplatin; Blastolem; Briplatin; Cisplatyl; Citoplatino; Citosin; Lederplatin; Metaplatin; Neoplatin; Placis; Platamine; Platiblastin; PlatiblastinS; Platinex; Platinol AQ; PlatinolAQ VHA Plus; Platiran; Platistin; Platosin.
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HS Tariff Code |
2843.90.0000
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不代表此产品 的实际溶解配方): 10% DMSO → 50% PEG300 → 5% Tween-80 → 35% ddH2O;假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄 清 DMSO 储备液加到 500 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入350 μL ddH2O定容至 1 mL); 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3328 mL | 16.6639 mL | 33.3278 mL | |
5 mM | 0.6666 mL | 3.3328 mL | 6.6656 mL | |
10 mM | 0.3333 mL | 1.6664 mL | 3.3328 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03558087 | Active Recruiting |
Drug: Nivolumab Drug: Cisplatin |
Bladder Cancer | Matthew Galsky | July 13, 2018 | Phase 2 |
NCT01670500 | Active Recruiting |
Drug: Cisplatin Drug: Doxorubicin |
Breast Cancer | Beth Israel Deaconess Medical Center |
October 2012 | Phase 2 |
NCT03809637 | Active Recruiting |
Drug: Pemetrexed, cisplatin | Yonsei University | Sarcoma | January 10, 2017 | Phase 2 |
NCT03345784 | Active Recruiting |
Drug: Cisplatin Drug: Adavosertib |
Cervical Carcinoma Vaginal Carcinoma |
National Cancer Institute (NCI) |
May 29, 2018 | Phase 1 |
NCT04003636 | Active Recruiting |
Drug: Cisplatin Drug: Placebo |
Biliary Tract Carcinoma | Merck Sharp & Dohme LLC | September 24, 2019 | Phase 3 |
The inhibition of tumor growth was enhanced by HemoHIM administration in melanoma-bearing mice which were injected with cisplatin.BMC Cancer.2009 Mar 17;9:85. th> |
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Growth inhibition effect of cisplatin and HemoHIM on melanoma cellsin vitro.BMC Cancer.2009 Mar 17;9:85. td> |
HemoHIM administration promotes immune responses for tumor surveillance in melanoma-bearing mice which were injected with cisplatin.BMC Cancer.2009 Mar 17;9:85. td> |