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Cisplatin/顺铂 {[allProObj[0].p_purity_real_show]}

货号:A210558 同义名: 顺-二胺二氯铂(II) / cis-Platinum; CDDP

Cisplatin (CDDP) 是一种抗肿瘤化疗剂,通过与 DNA 交联引起癌细胞中的 DNA 损伤。Cisplatin 可激活铁死亡 (ferroptosis) 并诱导自噬 (autophagy)。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Cisplatin/顺铂 化学结构 CAS号:15663-27-1
Cisplatin/顺铂 化学结构
CAS号:15663-27-1
Cisplatin/顺铂 3D分子结构
CAS号:15663-27-1
Cisplatin/顺铂 化学结构 CAS号:15663-27-1
Cisplatin/顺铂 3D分子结构 CAS号:15663-27-1
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Cisplatin/顺铂 生物活性

靶点
  • DNA synthesis

描述 Cisplatin (CDDP) is an antineoplastic chemotherapy agent, primarily by forming cross-links with DNA and thus inflicting DNA damage within cancer cells. Cisplatin triggers ferroptosis and induce autophagy, contributing to its effectiveness against various cancer types[1].[2].[3].
体内研究

In a study involving melanoma-bearing mice, Cisplatin administration (4 mg/kg B.W.) effectively reduced the size and weight of solid tumors. Moreover, supplementing Cisplatin treatment with HemoHIM further decreased both tumor size and weight, highlighting a potential synergistic effect[3].

Cisplatin treatment also results in notable adverse effects on kidney function, as demonstrated in a study where its administration significantly increased kidney weight as a percentage of total body weight, urine volume, serum creatinine, and blood urea nitrogen levels by approximately 132, 315, 797, and 556%, respectively, compared to control rats[4].

体外研究

When applied to HeLa cells, Cisplatin induces apoptosis in a dose-dependent manner, with a 30 μM concentration leading to the death of over 90% of the cells within 24 hours of treatment. Investigations into the kinetics of Cisplatin-induced apoptosis at this concentration have revealed that it activates the MEK/ERK signaling pathway. Notably, both 20 and 30 μM concentrations of Cisplatin significantly induce apoptosis and lead to a robust activation of ERK[1].

Cisplatin, at a 50 μM concentration, induces apoptosis in renal proximal tubular cells (RPTCs) in a time-dependent manner. This process is marked by cellular shrinkage, a 50-fold increase in caspase 3 activity, a fourfold rise in phosphatidylserine externalization, and significant increases in chromatin condensation and DNA hypoploidy by 5- and 15-fold, respectively[2].

Cisplatin/顺铂 细胞实验

Cell Line
Concentration Treated Time Description References
Murine proximal tubular epithelial cells (TKPTs) 20 µM 24 hours To investigate the effect of UNC0379 on cisplatin-induced apoptosis, results showed that UNC0379 reduced the number of TUNEL-positive cells, restored PTEN expression, and decreased cleaved caspase 3 levels. Cell Death Dis. 2025 Mar 31;16(1):226.
H1975 cells 20 μM 24 hours To evaluate the effect of KW6002 on cisplatin-induced DNA damage, results showed KW6002 increased cisplatin-induced DNA damage. J Clin Invest. 2022 Nov 15;132(22):e152924.
LLC1 cells 2 μM 24 hours To evaluate the effect of KW6002 on cisplatin-induced apoptosis, results showed KW6002 potentiated the efficacy of cisplatin. J Clin Invest. 2022 Nov 15;132(22):e152924.
RPTEC/hTERT1 cells 50 μM 48 hours To evaluate the effect of KW6002 on cisplatin-induced cell death, results showed KW6002 concentration-dependently reduced cisplatin-induced cell death. J Clin Invest. 2022 Nov 15;132(22):e152924.
HSC4 5 μM 9 days Generate cisplatin-tolerant persister cells (DTP cells) and observe high expression of FSP1 and lipid metabolism-related targets Aging (Albany NY). 2024 Jan 10;16(1):627-647.
HSC3 5 μM 9 days Generate cisplatin-tolerant persister cells (DTP cells) and observe high expression of FSP1 and lipid metabolism-related targets Aging (Albany NY). 2024 Jan 10;16(1):627-647.
osteoclasts 1.56 µmol/L 48 hours To evaluate the apoptosis-inducing ability of DZ(1:1)@ALN on osteoclasts, results showed that DZ(1:1)@ALN induced 64.20% apoptotic cells. Acta Pharm Sin B. 2020 Dec;10(12):2384-2403
RAW 264.7 cells 1.56 µmol/L 48 hours To evaluate the apoptosis-inducing ability of DZ(1:1)@ALN on RAW 264.7 cells, results showed that DZ(1:1)@ALN induced 68.10% apoptotic cells. Acta Pharm Sin B. 2020 Dec;10(12):2384-2403
MDA-MB-231 cells 3.125 µmol/L 48 hours To evaluate the apoptosis-inducing ability of DZ(1:1)@ALN on MDA-MB-231 cells, results showed that DZ(1:1)@ALN induced 42.7% apoptotic cells. Acta Pharm Sin B. 2020 Dec;10(12):2384-2403
Primary patient-derived ovarian cancer cells 20 µg/mL 2 hours DIPH and its derivatives increased DNA platination levels Mol Oncol. 2020 Apr;14(4):686-703
Res2-Igrov1 ovarian cancer cells 20 µg/mL 3 hours DIPH significantly increased CP-mediated DNA damage and apoptosis Mol Oncol. 2020 Apr;14(4):686-703
A2780res ovarian cancer cells 20 µg/mL 3 hours Measure DNA platination levels after CP exposure, found DIPH and its derivatives significantly increased DNA platination Mol Oncol. 2020 Apr;14(4):686-703
A2780 ovarian cancer cells 20 µg/mL 3 hours Measure DNA platination levels after CP exposure, found DIPH and its derivatives significantly increased DNA platination Mol Oncol. 2020 Apr;14(4):686-703
SKOV3 3.3 µM 24 h Generate cisplatin-resistant cell lines and validate cisplatin resistance Nat Commun. 2022 Aug 5;13(1):4554.
OVCAR5 3.3 µM 24 h Generate cisplatin-resistant cell lines and validate cisplatin resistance Nat Commun. 2022 Aug 5;13(1):4554.
COV362 3.3 µM 24 h Generate cisplatin-resistant cell lines and validate cisplatin resistance Nat Commun. 2022 Aug 5;13(1):4554.
N-DNA 3.3 mM 1 h To investigate the effect of Cisplatin on N-DNA, it was found that Cisplatin could effectively fix the N-DNA structure even under 180 mM NaCl conditions. Nucleic Acids Res. 2021 Dec 2;49(21):12035-12047.
N-DNA 0.1 mM To investigate the effect of low concentration Cisplatin on N-DNA, it was found that even low concentration Cisplatin could partially fix the N-DNA structure. Nucleic Acids Res. 2021 Dec 2;49(21):12035-12047.
T24 0-100 μM 3 days To evaluate the cytotoxicity of cisplatin in bladder cancer cell lines, T24 cells exhibited the lowest sensitivity to cisplatin. Mol Cancer. 2022 Feb 7;21(1):37.
T24 0.25 μM 7 or 14 days Genome-wide CRISPR screening identified HNRNPU as the top candidate gene related to cisplatin resistance. Mol Cancer. 2022 Feb 7;21(1):37.

Cisplatin/顺铂 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nu/nu mice Subcutaneous xenograft model Intraperitoneal injection 5 mg/kg Once per week for 2-3 weeks SQLE depletion significantly inhibited tumor growth, and the combination with cisplatin exhibited a more robust inhibitory effect than cisplatin alone Adv Sci (Weinh). 2023 Sep;10(27):e2206878.
BALB/c nu/nu mice Subcutaneous xenograft model Intraperitoneal injection 5 mg/kg Once per week for four weeks SQLE knockdown reduced tumor size, weight, and volume, with a more pronounced effect when combined with cisplatin. Adv Sci (Weinh). 2023 Sep;10(27):e2206878.
CD-1 Nu/Nu mice A2780-CP20 ovarian cancer xenograft model Intravenous injection 4 mg/kg/day APR-246 for 7 consecutive days, cisplatin on days 2 and 6 Combination treatment with APR-246 and cisplatin significantly inhibited tumor growth by 56% and was well tolerated. Cell Death Dis. 2015 Jun 18;6(6):e1794.
BALB/c-nu/nu mice Breast cancer bone metastasis model Intravenous injection 0.25 mg/kg Every six days for a total of three injections To evaluate the inhibitory effect of DZ(1:1)@ALN on tumor growth and osteolysis in vivo, results showed that DZ(1:1)@ALN significantly inhibited tumor growth and osteolysis without inducing obvious systemic toxicity. Acta Pharm Sin B. 2020 Dec;10(12):2384-2403
Mice Patient-derived xenograft model (PDX) Intraperitoneal injection 10 mg/kg Weekly for 3 weeks Validate the effect of FAO inhibitor combined with platinum drugs on cisplatin-resistant tumors Nat Commun. 2022 Aug 5;13(1):4554.
BALB/c nu/nu female mice Tumor xenograft model Tail injection 2 mg/kg Every other day for 4 weeks To validate the effect of HNRNPU knockout on cisplatin sensitivity in vivo, results showed that HNRNPU knockout significantly enhanced cisplatin sensitivity. Mol Cancer. 2022 Feb 7;21(1):37.

Cisplatin/顺铂 动物研究

Animal study 肾损伤[5]
动物:C57BL/6小鼠,雄性,8-12周龄。
给药:25 mg/kg,腹腔注射。

Cisplatin/顺铂 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
NCT02128282 Cholangiocarcinoma Phase 1 Phase 2 Recruiting November 2021 United States, Arizona ... 展开 >> Mayo Clinic Recruiting Scottsdale, Arizona, United States, 85259-5499 Contact: Mayo Clinic Clinical Trials Office    855-776-0015       Principal Investigator: Mitesh Borad, M.D.          United States, Colorado University of Colorado- Denver Recruiting Aurora, Colorado, United States, 80045 Contact: Amy Szilard    720-848-0702    Amy.Szilard@ucdenver.edu    Principal Investigator: Sarah (Lindsey) Davis, MD          United States, Florida Mayo Clinic Recruiting Jacksonville, Florida, United States, 32224 Contact: Mayo Clinic Clinical Trials Office    855-776-0015       Principal Investigator: Kabir Mody, MD          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Mayo Clinic Clinical Trials Office    855-776-0015       Principal Investigator: Joleen Hubbard, MD          United States, Texas Texas Oncology - Baylor Charles A. Sammons Cancer Center Recruiting Dallas, Texas, United States, 75246 Contact: Tammy Carmical, RN    214-370-1937    tammy.carmical@usoncology.com    Principal Investigator: Carlos Becerra, M.D.          Texas Oncology-Tyler Recruiting Tyler, Texas, United States, 75702 Contact: Karen Poe, RN    903-579-9869    karen.poe@usoncology.com    Principal Investigator: Donald A Richards, M.D.          Korea, Republic of Asan Medical Center Recruiting Seoul, Songpa-gu, Korea, Republic of, 138-736 Contact: Heung-Moon Chang, MD    82-3010-3219 ext 3210    changhm@amc.seoul.kr    Contact: Seok kyung Jeong    82-2-3010-5634    jsk0213@amc.seoul.kr    Samsung Medical Center Recruiting Seoul, Korea, Republic of Contact: Eunyou Lee    82-2-3410-0955    ley0709@samsung.com    Principal Investigator: Joon Oh Park, MD          Seoul National University Hospital Recruiting Seoul, Korea, Republic of Contact: Myoungsun Choi    82-2-2072-7612    iamyou3@hanmail.net    Principal Investigator: Do-Youn Oh, MD          Severance Hospital, Yonsei University Health System Recruiting Seoul, Korea, Republic of Contact: So Young Hwang    82-2-2228-8180    syhwang@yuhs.ac    Principal Investigator: Sun Young Rha, MD          Taiwan China Medical University Hospital Recruiting Taichung City, Taiwan Contact: Pei-Chen Hsu    +886-4-2205-2121    peggyshiu0807@gmail.com    Principal Investigator: Li-Yuan Bai, M.D. 收起 <<
NCT00915382 Advanced Gastric Cancer Phase 3 Completed - Korea, Republic of ... 展开 >> Department of Oncology, Asan Medical Center Seoul, Korea, Republic of, 138-736 收起 <<
NCT03427359 Nasopharyngeal Carcinoma Phase 2 Completed - -

Cisplatin/顺铂 参考文献

[1]Wang X, et al. Requirement for ERK activation in cisplatin-induced apoptosis. J Biol Chem. 2000 Dec 15;275(50):39435-43.

[2]Cummings BS, et al. Cisplatin-induced renal cell apoptosis: caspase 3-dependent and -independent pathways. J Pharmacol Exp Ther. 2002 Jul;302(1):8-17.

[3]Park HR, et al. Enhanced antitumor efficacy of cisplatin in combination with HemoHIM in tumor-bearing mice. BMC Cancer. 2009 Mar 17;9:85.

[4]Shimeda Y, et al. Protective effects of capsaicin against cisplatin-induced nephrotoxicity in rats. Biol Pharm Bull. 2005 Sep;28(9):1635-8.

[5]Williams RM, Shah J, Mercer E, Tian HS, Thompson V, Cheung JM, Dorso M, Kubala JM, Gudas LJ, de Stanchina E, Jaimes EA, Heller DA. Kidney-Targeted Redox Scavenger Therapy Prevents Cisplatin-Induced Acute Kidney Injury. Front Pharmacol. 2022 Jan 3;12:790913.

Cisplatin/顺铂 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.66mL

3.33mL

1.67mL

33.33mL

6.67mL

3.33mL

Cisplatin/顺铂 技术信息

CAS号15663-27-1
分子式Cl2H6N2Pt
分子量 300.05
SMILES Code Cl[Pt]Cl.N.N
MDL No. MFCD00011623
别名 顺-二胺二氯铂(II) ;cis-Platinum; CDDP; CACP; cis-Diamminedichloroplatinum; DDP; cis DDP; cis-diamminedichloroplatinum II; NSC 119875; cis-Diaminodichloroplatinum
运输蓝冰
InChI Key DQLATGHUWYMOKM-UHFFFAOYSA-L
Pubchem ID 2767
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,2-8°C

溶解方案

H2O: 1 mg/mL(3.33 mM),配合低频超声,并水浴加热至45℃助溶

DMF: 10 mg/mL(33.33 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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