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.
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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。 |
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]. |
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 << |
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 |
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 |