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络铂 /Lobaplatin {[allProObj[0].p_purity_real_show]}

货号:A657863 同义名: D-19466

Lobaplatin is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links.

Lobaplatin 化学结构 CAS号:135558-11-1
Lobaplatin 化学结构
CAS号:135558-11-1
Lobaplatin 3D分子结构
CAS号:135558-11-1
Lobaplatin 化学结构 CAS号:135558-11-1
Lobaplatin 3D分子结构 CAS号:135558-11-1
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Lobaplatin 纯度/质量文件 产品仅供科研

货号:A657863 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Bax Bcl-2 Bcl-B Bcl-w Bcl-xL Bfl-1 Mcl-1 其他靶点 纯度
BTSA1 99%+
HA14-1 +

Bcl-2, IC50: 9 μM

98%
Venetoclax ++++

Bcl-2, Ki: <0.01 nM

99%
Navitoclax 99%+
Obatoclax Mesylate +++

Bcl-2, Ki: 0.22 μM

98%
ABT-737 +++

Bcl-2, EC50: 30.3 nM

+

Bcl-B, EC50: 1.82 μM

+++

Bcl-w, EC50: 197.8 nM

+++

Bcl-xL, EC50: 78.7 nM

99%+
Gambogic Acid +

Bfl-1, IC50: 1.06 μM

Bcl-2, IC50: 1.21 μM

++

Bcl-B, IC50: 0.66 μM

++++

Bcl-w, IC50: 0.02 μM

+

Bcl-xL, IC50: 1.47 μM

+

Bfl-1, IC50: 1.06 μM

++

Mcl-1, IC50: 0.79 μM

Caspase 99% HPLC
BH3I-1 +

BH3-Bcl-xL interaction, Ki: 2.4 μM

98%
A-1331852 ++++

Bcl-xL, Ki: <0.01 nM

99%+
A-1210477 ++++

MCL-1, IC50: 26.2 nM

99%+
Maritoclax 97%
TW-37 +++

Bcl-2, Ki: 0.29 μM

+

Bcl-xL, Ki: 1.11 μM

+++

Mcl-1, Ki: 0.26 μM

98%
UMI-77 ++

Mcl-1, Ki: 490 nM

97%
(R)-(-)-Gossypol acetic acid ++

Bcl-2, Ki: 0.32 μM

++

Bcl-xL, Ki: 0.48 μM

+++

Mcl-1, Ki: 0.18 μM

98%
Sabutoclax ++

Bfl-1, IC50: 0.62 μM

Bcl-2, IC50: 0.32 μM

++

Bcl-xL, IC50: 0.31 μM

++

Bfl-1, IC50: 0.62 μM

+++

Mcl-1, IC50: 0.20 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Capase-7 Caspase Caspase-1 Caspase-10 Caspase-2 Caspase-3 Caspase-4 Caspase-5 Caspase-6 Caspase-8 Caspase-9 其他靶点 纯度
Emricasan 99%+
Z-VAD(OMe)-FMK 99%+
Z-VAD-FMK 99%+
Q-VD-OPh 97%
VX-765 ++++

Caspase-1, Ki: 0.8 nM

++++

Caspase-4, Ki: <0.6 nM

99%+
Ac-DEVD-CHO +++

caspase-7, Ki: 1.6 nM

+++

Caspase-1, Ki: 18 nM

+++

caspase-10, Ki: 12 nM

+

caspase-2, Ki: 1.71 μM

++++

Caspase-3, Ki: 230 pM

++

Caspase-4, Ki: 132 nM

++

caspase-5, Ki: 205 nM

+++

caspase-6, Ki: 31 nM

++++

caspase-8, Ki: 0.92 nM

++

Caspase-9, Ki: 60 nM

98%+
Z-DEVD-FMK 98%
Z-IETD-FMK 98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Lobaplatin 生物活性

描述 Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation[3]. Lobaplatin and paclitaxel inhibited SGC-7901 cell growth in a concentration and timedependent manner, with IC25 values at 48h of 1.97±0.17µg/ml and 1.98±0.19 ng/ml, respectively. Lobaplatin did not affect cyclin D1 and CDK4 protein expression, while cyclin E1 and CDK2 levels were significantly increased, with cyclin B1 amounts markedly decreased (p<0.05). More S phase cells were observed after lobaplatin treatment compared with controls (60.03±1.25 vs. 18.69±0.96%; p<0.05). Lobaplatin and paclitaxel combination did not affect cyclin D1 and CDK4 protein levels (p>0.05); meanwhile, cyclin E1 and CDK2 levels were increased, with reduced cyclin B1 amounts, compared with control values (p<0.05)[4].Lobaplatin inhibited proliferation of human HCC cells in a dose-dependent manner. For the most sensitive SMMC-7721 cells, lobaplatin arrested cell cycle progression in G1 and G2/M phases time-dependently which might be associated with the down-regulation of cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and the up-regulation of p53, p21, and p27[5].Lobaplatin inhibited the proliferation of human gastric cancer cells and induced apoptosis, which may be associated with the up-regulation of Bax expression, poly(ADP-ribose) polymerase (PARP) cleavage, p53 expression and the reduction of Bcl-2 expression[6].

Lobaplatin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03731442 Esophageal Cancer Phase 3 Recruiting October 31, 2027 China, Beijing ... 展开 >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD 收起 <<
NCT03328234 IMRT With or Without Concurren... 展开 >>t Chemotherapy for Esophageal Cancer 收起 << Phase 3 Recruiting December 31, 2022 China ... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, China, 100021 Contact: Xin Wang, MD    +861013311583220    beryl_wx2000@163.com 收起 <<
NCT03308552 Esophageal Neoplasms Phase 3 Recruiting August 30, 2021 China, Beijing ... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD 收起 <<

Lobaplatin 参考文献

[1]Welink J, Boven E, et al. Pharmacokinetics and pharmacodynamics of lobaplatin (D-19466) in patients with advanced solid tumors, including patients with impaired renal of liver function. Clin Cancer Res. 1999 Sep;5(9):2349-58.

[2]Gietema JA, Veldhuis GJ, et al. Phase II and pharmacokinetic study of lobaplatin in patients with relapsed ovarian cancer. Br J Cancer. 1995 Jun;71(6):1302-7.

[3] M J McKeage. Lobaplatin: a new antitumour platinum drug. Expert Opin Investig Drugs. 2001 Jan;10(1):119-28.

[4] Suhang Hua,et al. Anticancer Mechanism of Lobaplatin as Monotherapy and in Combination with Paclitaxel in Human Gastric Cancer. Curr Mol Pharmacol. 2018;11(4):316-325.

[5]Qiong Wu,et al. Lobaplatin arrests cell cycle progression in human hepatocellular carcinoma cells. J Hematol Oncol. 2010 Oct 31;3:43.

[6]Chu-Yang Yin,et al. Lobaplatin inhibits growth of gastric cancer cells by inducing apoptosis. World J Gastroenterol.2014 Dec 14;20(46):17426-33.

Lobaplatin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

Lobaplatin 技术信息

CAS号135558-11-1
分子式C9H18N2O3Pt
分子量 397.329
别名 D-19466
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

H2O: 50 mg/mL(125.84 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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