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  3. Ferroptosis inducer-9

Ferroptosis inducer-9 是一种铁死亡 (ferroptosis) 诱导剂和秋水仙碱结合位点微管蛋白 (tubulin) 聚合抑制剂。Ferroptosis inducer-9 以 IC50 为 14 nM 抑制 MCF-7 细胞生长,并抑制 [3H]colchicine 结合。Ferroptosis inducer-9 可降低 GPX4FTH 的表达,提高 COX2ACSL4,降低 GSHNADP+NADPH 水平,提高 LPOMDAFe(II) 水平,并降低 SOD 浓度。Ferroptosis inducer-9 在 HCT116 CRC 异种移植瘤模型中表现出显著的抗肿瘤功效。Ferroptosis inducer-9 可用于研究三阴性乳腺癌 (TNBC) 和结直肠癌 (CRC)。

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Ferroptosis inducer-9

Ferroptosis inducer-9 Chemical Structure

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生物活性

Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC)[1].

体外研究
(In Vitro)

Ferroptosis inducer-9 (Compound 12) 抑制微管蛋白聚合 (IC50 = 550 nM) 并抑制 MCF-7 细胞生长 (IC50 = 14 nM)[1]
Ferroptosis inducer-9 (0.3-1 μM) 可导致 H2BC11-moxGFP/sTagRFP-TUBA1B 标记的 MDA-MB-231 细胞完全生长停滞,并引起显著的细胞核和细胞骨架形态改变[1]
Ferroptosis inducer-9 (72 h) 可抑制 SW620、SW480、HCT116、HepG2 和 CC-2509f 细胞的生长,其 IC50 值分别为 0.633 μM、0.0654 μM、0.389 μM、107.3 μM、52.9 μM[1]
Ferroptosis inducer-9 可下调 HCT116 细胞中铁死亡抑制因子 (SLC7A11、SLC3A2、SLC11A2、NRF2、NCOA4、KEAP1、GPX4、FTL、FTH1) 的表达,并上调铁死亡促进因子 (PTGS2、NOX1、COX2、COX4、ACSL4) 的表达[1]
Ferroptosis inducer-9 可降低 GSH 和 SOD 浓度,降低 NADP+ 和 NADPH 浓度,提高 LPO、MDA 和 Fe(II) 水平以及 GSSG 浓度[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ferroptosis inducer-9 (Compound 12) (25 mg/kg,腹腔注射,每 2 天一次,持续 30 天) 在携带 HCT116 结直肠癌异种移植瘤的裸鼠中显示出显著的抗肿瘤作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCT116 colorectal cancer cells (1×108 cells/mL in logarithmic growth phase) were subcutaneously implanted into the flanks of 10-week-old male BALB/C mice[1]
Dosage: 25 mg/kg
Administration: intraperitoneal injection, once every 2 days for 30 days
Result: Achieved tumor growth inhibition.
Reduced the Ki67 expression.
分子量

410.44

Formula

C21H18N2O5S

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.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ferroptosis inducer-9
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HY-175698
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