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Oxaliplatin/奥沙利铂 {[allProObj[0].p_purity_real_show]}

货号:A100048 同义名: Lipoxal; RP 54780

Oxaliplatin是一种 DNA 合成抑制剂,通过诱导 DNA 交联损伤阻止 DNA 复制和转录,导致细胞死亡。Oxaliplatin 以时间依赖方式抑制人黑色素瘤细胞系 C32 和 G361,其 IC50 值分别为 0.98 μM 和 0.14 μM,同时还可诱导细胞自噬 (autophagy)。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Oxaliplatin/奥沙利铂 化学结构 CAS号:61825-94-3
Oxaliplatin/奥沙利铂 化学结构
CAS号:61825-94-3
Oxaliplatin/奥沙利铂 3D分子结构
CAS号:61825-94-3
Oxaliplatin/奥沙利铂 化学结构 CAS号:61825-94-3
Oxaliplatin/奥沙利铂 3D分子结构 CAS号:61825-94-3
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Oxaliplatin/奥沙利铂 纯度/质量文件 产品仅供科研

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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Oxolinic acid 98+%
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 95%
Favipiravir 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

98%
SU056 +

YB-1, IC50: 1.73 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。

Oxaliplatin/奥沙利铂 生物活性

靶点
  • DNA synthesis

描述 DNA damage is an abnormal chemical structure in DNA, while a mutation is a change in the sequence of standard base pairs. Oxaliplatin is an alkylating agent that inhibits DNA synthesis and replication by generating DNA damage[1]. Oxaliplatin can induces immunogenic cell death by provoking the presentation of damage associated molecular patterns. Oxaliplatin inhibited human colorectal tumor cell lines HCT-8, HT-29 and HCT 116 with IC50 values of 0.87 μM, 0.88 μM and 0.53 μM, respectively[2]. Oxaliplatin inhibited human bladder cancer cell lines TCC SUP and RT-4 with IC50 values of 15.04 and 11.10 μM, respectively. Oxaliplatin inhibited human Glioma cell lines U-87MG and U-373MG with IC50 values of 17.60 and 2.95 μM, respectively[3]. Furthermore, oxaliplatin could active mTOR pathway via increasing the level of phosphorylated p70 S6 kinase in five ATCC cell lines HCT15, DLD-1, LoVo, HCT116, HT29 and Colo 205[4]. In vivo, administration of 10 mg/kg Oxaliplatin via tail vein injection once a week for 4 weeks significantly inhibited the MHCC97 cells subcutaneously tumor[5]. Treatment with Oxaliplatin at the dose of 10 mg/kg once a week for 4 weeks inhibited the growth of human hepatocellular HCCLM3 xenografts in nude mice[6]. Treatment with oxaliplatin at the dose of 10 mg/kg induced mTOR activation and immunogenic cell death in colon cancer xenografts model. In early clinical, oxaliplatin demonstrated clinical activity in a variety of tumors, including CRC, breast, endometrial cancers and malignant melanoma[7].

Oxaliplatin/奥沙利铂 细胞实验

Cell Line
Concentration Treated Time Description References
HT29-OR cells 10 µM 4 hours To evaluate the effect of BML-277 on CHK2 activity and protein PARylation, results showed that BML-277 attenuated CHK2 activity, protein PARylation and FANCD2 monoubiquitination. Br J Cancer. 2022 Nov;127(9):1615-1628.
DLD-1 cells 100 μM 6 hours To investigate the effect of oxaliplatin and cetuximab on DUOX2 mRNA levels. Results showed that oxaliplatin significantly upregulated DUOX2 mRNA levels, while cetuximab inhibited this upregulation. J Natl Cancer Inst. 2015 Dec 30;108(6):djv394.
SW48 cells 50 μM 6 hours To investigate the effect of oxaliplatin and cetuximab on DUOX2 mRNA levels. Results showed that oxaliplatin significantly upregulated DUOX2 mRNA levels, while cetuximab inhibited this upregulation. J Natl Cancer Inst. 2015 Dec 30;108(6):djv394.
Mouse dorsal root ganglion sensory neurons 25–50 μM 10–20 minutes To evaluate the effect of Benztropine on oxaliplatin-induced neuronal excitability changes. Results showed that Benztropine significantly reversed oxaliplatin-induced membrane depolarization, reduced action potential peak amplitude, and increased rise and decay times. Acta Neuropathol Commun. 2019 Jan 18;7(1):9.
Primary culture of rat Schwann cells 3 μM 48 hours To assess oxaliplatin's effect on HMGB1 release from Schwann cells J Neuroinflammation. 2019 Oct 30;16(1):199.
Macrophage-like RAW264.7 cells 10 μM 24 hours To evaluate oxaliplatin-induced HMGB1 release J Neuroinflammation. 2019 Oct 30;16(1):199.
Mouse dorsal root ganglion neurons 100 μM 24 hours To evaluate the effect of oxaliplatin on TRPM3 channel activity. Results showed that oxaliplatin pretreatment significantly increased PS-induced calcium influx and high K+-induced calcium influx. Pain. 2023 Sep 1;164(9):2060-2069
HEK293T cells stably expressing human TRPM3 100 μM 24 hours To evaluate the effect of oxaliplatin on TRPM3 channel activity. Results showed that oxaliplatin pretreatment significantly increased PS or heat-induced calcium influx. Pain. 2023 Sep 1;164(9):2060-2069
HEK293T cells stably expressing murine TRPM3 100 μM 24 hours To evaluate the effect of oxaliplatin on TRPM3 channel activity. Results showed that oxaliplatin pretreatment significantly increased basal calcium levels and PS or heat-induced calcium influx. Pain. 2023 Sep 1;164(9):2060-2069
CRC PDOs 0 to 100 μM 7 days To evaluate the sensitivity of Oxaliplatin to CRC PDOs, the results showed that Oxaliplatin significantly inhibited the growth of PDOs Cell Death Dis. 2022 Apr 5;13(4):303.
HCT116 cells 40 µM 24 h To evaluate the effect of NFS1 deficiency combined with oxaliplatin on cell death, the results showed that NFS1 deficiency significantly enhanced the antitumor effect of oxaliplatin and induced PANoptosis (apoptosis, necroptosis, pyroptosis, and ferroptosis). Signal Transduct Target Ther. 2022 Feb 28;7(1):54.
DLD1 cells 80 µM 24 h To evaluate the effect of NFS1 deficiency combined with oxaliplatin on cell death, the results showed that NFS1 deficiency significantly enhanced the antitumor effect of oxaliplatin and induced PANoptosis (apoptosis, necroptosis, pyroptosis, and ferroptosis). Signal Transduct Target Ther. 2022 Feb 28;7(1):54.
HT29 0.1 μM to 1.0 μM 2–3 months To generate oxaliplatin-resistant CRC cell lines and evaluate their sensitivity to oxaliplatin. Results showed that oxaliplatin-resistant cell lines had reduced sensitivity to oxaliplatin. Br J Cancer. 2022 Nov;127(9):1615-1628.
HT29-OR 1.0 μM To evaluate the tumor sphere formation ability of oxaliplatin-resistant cell lines in a 3D environment and analyze their protein kinase phosphorylation levels. Results showed that the phosphorylation level of CHK2 at Thr68 was significantly elevated in HT29-OR cells. Br J Cancer. 2022 Nov;127(9):1615-1628.
RKO cells 62.5 µg/mL 24 h To evaluate the effect of oHA on oxaliplatin sensitivity, results showed that the combination of oHA with oxaliplatin significantly increased the apoptosis rate. Drug Deliv. 2021 Dec;28(1):920-929.
RKO cells 125 µg/mL 24 h To evaluate the effect of oHA on oxaliplatin sensitivity, results showed that the combination of oHA with oxaliplatin significantly increased the apoptosis rate. Drug Deliv. 2021 Dec;28(1):920-929.
RKO cells 250 µg/mL 24 h To evaluate the effect of oHA on oxaliplatin sensitivity, results showed that the combination of oHA with oxaliplatin significantly increased the apoptosis rate. Drug Deliv. 2021 Dec;28(1):920-929.

Oxaliplatin/奥沙利铂 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice (nu/nu) DLD-1 xenograft model Intraperitoneal injection 8 mg/kg 24 hours To investigate the effect of oxaliplatin and cetuximab on DUOX2 and DUOXA2 mRNA levels. Results showed that oxaliplatin significantly upregulated DUOX2 and DUOXA2 mRNA levels, while cetuximab inhibited this upregulation. J Natl Cancer Inst. 2015 Dec 30;108(6):djv394.
Nude mice Xenograft mice model Intrapulmonary injection 1 mg/kg Once daily for 21 days JW55, as a β-Catenin inhibitor, enhanced the inhibitory effect of AR-CS on the proliferation and migration of SW620 cells when used in combination Chin Med. 2022 Jan 6;17(1):11
BALB/c nude mice CRC xenograft tumors Intraperitoneal injection 5 mg/kg Once a week for 14 days To evaluate the therapeutic effect of Oxaliplatin on CRC xenograft tumors, the results showed that Oxaliplatin significantly inhibited tumor growth Cell Death Dis. 2022 Apr 5;13(4):303.
Mice Oxaliplatin-induced neuropathic pain model Intraperitoneal injection 2.4 mg/kg Days 1, 2, 5-9, 12-14, total of 10 injections To evaluate the pain response in the oxaliplatin-induced neuropathic pain model in mice and validate the analgesic effects of drugs through behavioral tests. J Med Chem. 2020 May 28;63(10):5185-5200
Nude mice CRC xenograft model Intraperitoneal injection 7.5 mg/kg Every 3 days for 30 days To evaluate the effect of NFS1 deficiency combined with oxaliplatin on tumor growth, the results showed that NFS1 deficiency significantly enhanced the antitumor effect of oxaliplatin and reduced tumor volume and weight. Signal Transduct Target Ther. 2022 Feb 28;7(1):54.
Mice MCA205 fibrosarcoma model Intraperitoneal injection 10 mg/kg To evaluate the effect of ISO combined with oxaliplatin on tumor growth, the results showed that the combination treatment significantly inhibited tumor growth, and this effect depended on the immune system. Cell Death Dis. 2020 Nov 26;11(11):1015.
Nude mice HCC xenograft model Intraperitoneally 5 mg/kg 3 times per week for 2 weeks Oxaliplatin treatment inhibited the growth of HCC xenograft tumors Cell Death Dis. 2023 Feb 2;14(2):79
NOD/SCID mice HT29 cell xenograft model Intraperitoneal injection 5 mg/kg Once a week for 3 weeks To evaluate the anti-tumor effect of oxaliplatin on HT29 cell xenograft models. Results showed that oxaliplatin significantly inhibited the growth of tumors carrying the empty vector, but had a lesser effect on tumors expressing CHK2-WT or CHK2-TD. Br J Cancer. 2022 Nov;127(9):1615-1628.
Nude mice RKO cell tumor model Tail vein injection 5 mg/kg Every 3 days for 5 times To evaluate the in vivo antitumor effect of oHA-Lipid-Oxa, results showed that oHA-Lipid-Oxa significantly inhibited tumor growth and reduced side effects. Drug Deliv. 2021 Dec;28(1):920-929.

Oxaliplatin/奥沙利铂 动物研究

Dose Mice: 2 mg/kg, 6 mg/kg[3] (i.p.), 5 mg/kg - 40 mg/kg[4] (i.p.), 3.5 mg/kg[5] (i.v.)
Rat[6] : 2.3 mg/kg - 5 mg/kg (i.v.), 30 mg/kg (p.o.)
Administration i.p., i.v., p.o.

Oxaliplatin/奥沙利铂 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
NCT01157052 Neoplasms, Colorectal ... 展开 >> Colorectal Cancer Colorectal Carcinoma 收起 << Phase 1 Unknown September 2015 Canada, Alberta ... 展开 >> Cross Cancer Institute Not yet recruiting Edmonton, Alberta, Canada, T6G 1Z2 Sub-Investigator: Judith Meza-Junco, MD 收起 <<
NCT00005856 Adult Giant Cell Glioblastoma ... 展开 >> Adult Glioblastoma Adult Gliosarcoma 收起 << Phase 1 Phase 2 Terminated(Administratively co... 展开 >>mplete.) 收起 << - United States, Maryland ... 展开 >> New Approaches to Brain Tumor Therapy Consortium Baltimore, Maryland, United States, 21231-1000 收起 <<
NCT01795027 Gastric Cancer Phase 3 Unknown June 2018 China, Guangdong ... 展开 >> the central hospital of Chaozhou Chaozhou, Guangdong, China the 1st people's hospital of Foshan Foshan, Guangdong, China cancer center of Guangzhou medical college Guangzhou, Guangdong, China cancer center of Sun yat-sen University Guangzhou, Guangdong, China Guangdong Traditional Medical Hospital Guangzhou, Guangdong, China the 1st affliated hospital of Guangdong pharmacuetic college Guangzhou, Guangdong, China the 1St Affliated Hospital of Guangzhou Medical College Guangzhou, Guangdong, China the 6th affliated hospital of Sun-yat-sen University Guangzhou, Guangdong, China the 1st hospital of Shantou University Shantou, Guangdong, China the cental hospital of Shantou Shantou, Guangdong, China YUE-BEI people's hospital Shaoguan, Guangdong, China the 2nd people's hospital of Shenzhen Shenzhen, Guangdong, China the 5th hospital of Sun-yat-sen University Zhuhai, Guangdong, China 收起 <<

Oxaliplatin/奥沙利铂 参考文献

[1]Arango D, Wilson AJ, Shi Q, Corner GA, Arañes MJ, Nicholas C, Lesser M, Mariadason JM, Augenlicht LH. Molecular mechanisms of action and prediction of response to oxaliplatin in colorectal cancer cells. Br J Cancer. 2004 Nov 29;91(11):1931-46. doi: 10.1038/sj.bjc.6602215. PMID: 15545975; PMCID: PMC2409767.

[2]Balin-Gauthier D, Delord JP, Rochaix P, Mallard V, Thomas F, Hennebelle I, Bugat R, Canal P, Allal C. In vivo and in vitro antitumor activity of oxaliplatin in combination with cetuximab in human colorectal tumor cell lines expressing different level of EGFR. Cancer Chemother Pharmacol. 2006 Jun;57(6):709-18. doi: 10.1007/s00280-005-0123-3. Epub 2005 Dec 1. PMID: 16320055.

[3]Rixe O, Ortuzar W, Alvarez M, Parker R, Reed E, Paull K, Fojo T. Oxaliplatin, tetraplatin, cisplatin, and carboplatin: spectrum of activity in drug-resistant cell lines and in the cell lines of the National Cancer Institute's Anticancer Drug Screen panel. Biochem Pharmacol. 1996 Dec 24;52(12):1855-65. doi: 10.1016/s0006-2952(97)81490-6. PMID: 8951344.

[4]Lu M, Zessin AS, Glover W, Hsu DS. Activation of the mTOR Pathway by Oxaliplatin in the Treatment of Colorectal Cancer Liver Metastasis. PLoS One. 2017 Jan 6;12(1):e0169439. doi: 10.1371/journal.pone.0169439. PMID: 28060954; PMCID: PMC5218497.

[5]Bu Y, Jia QA, Ren ZG, Zhang JB, Jiang XM, Liang L, Xue TC, Zhang QB, Wang YH, Zhang L, Xie XY, Tang ZY. Maintenance of stemness in oxaliplatin-resistant hepatocellular carcinoma is associated with increased autocrine of IGF1. PLoS One. 2014 Mar 14;9(3):e89686. doi: 10.1371/journal.pone.0089686. PMID: 24632571; PMCID: PMC3954560.

[6]Wang Z, Zhou J, Fan J, Qiu SJ, Yu Y, Huang XW, Sun J, Tan CJ, Dai Z. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604. doi: 10.1517/13543780903292626. PMID: 19780708.

[7]Misset JL, Bleiberg H, Sutherland W, Bekradda M, Cvitkovic E. Oxaliplatin clinical activity: a review. Crit Rev Oncol Hematol. 2000 Aug;35(2):75-93. doi: 10.1016/s1040-8428(00)00070-6. PMID: 10936465.

Oxaliplatin/奥沙利铂 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

12.59mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

Oxaliplatin/奥沙利铂 技术信息

CAS号61825-94-3
分子式C8H14N2O4Pt
分子量 397.29
SMILES Code O=C1O[Pt]2([NH2][C@@H]3CCCC[C@H]3[NH2]2)OC1=O
MDL No. MFCD00866327
别名 Lipoxal; RP 54780; LOHP; Eloxatine; NSC 266046
运输蓝冰
InChI Key DRMCATBEKSVAPL-BNTLRKBRSA-N
Pubchem ID 9887053
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

H2O: 2 mg/mL(5.03 mM),配合低频超声,并水浴加热至45℃助溶

DMF: 1.5 mg/mL(3.78 mM),配合低频超声助溶

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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