Antitumor agent-36

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Antitumor agent-36 

Antitumor agent-36 具有有效的抗增殖和抗转移活性。Antitumor agent-36 诱导严重的 DNA 损伤并进一步导致 γ-H2AX 和 p53 的高表达。Antitumor agent-36 通过线粒体凋亡通路 Bcl-2/Bax/caspase3 促进肿瘤细胞凋亡 (apoptosis)。Antitumor agent-36 通过抑制 PD-L1 的表达以增加肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞显著改善免疫反应。

Antitumor agent-36

Antitumor agent-36 Chemical Structure

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生物活性

Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues[1].

IC50 & Target

apoptosis[1]
体外研究
(In Vitro)

Antitumor agent-36 (compound 1) (24-76 hours) displays relatively lower activities after 24 h treatment, and the IC50 values decreases at 48 h, and the activities at 72 h are similar to that of 48 h[1].
Antitumor agent-36 (compound 1) (24 hours) induces significant apoptosis of tumor cells.[1].
Antitumor agent-36 (compound 1) (24 hours) are effective in modulating the expression of apoptotic proteins in tumor cells [1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: murine tumor cell line 4T1 and human tumor cell line A549
Concentration: 5 and 10 μM
Incubation Time: 24 hours
Result: Exhibited effective apoptosis induction of both A549 and 4T1 cells after 24 h treatment.

分子量

804.58

Formula

C32H30Cl2N2O6Pt
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Li Z, et al. Ketoprofen and Loxoprofen Platinum(IV) Complexes Displaying Antimetastatic Activities by Inducing DNA Damage, Inflammation Suppression, and Enhanced Immune Response. J Med Chem. 2021;64(24):17920-17935.

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