2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. MDM-2/p53 Apoptosis Reactive Oxygen Species
  4. Anticancer agent 42

Anticancer agent 42 (化合物10d) 是一种口服有效的抗癌剂，对 MDA-MB-231 细胞具有较强的抗肿瘤活性，其 IC50 为 0.07 μM。Anticancer agent 42 通过激活凋亡通路和 p53 表达发挥抗癌作用。Anticancer agent 42 可用于转移性乳腺癌的研究。

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Anticancer agent 42 Chemical Structure

Anticancer agent 42 Chemical Structure

CAS No. : 2687265-18-3

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Anticancer agent 42 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer[1].

IC50 & Target

IC50: 0.07 μM (Anticancer in MDA-MB-231 cell)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.21 μM
Compound: 10d
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay
[PMID: 35477142]
HeLa IC50
0.32 μM
Compound: 10d
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
[PMID: 35477142]
MDA-MB-231 IC50
0.07 μM
Compound: 10d
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
[PMID: 35477142]
体外研究
(In Vitro)

Anticancer agent 42 (compound 10d) (0-20 μM, 4 h) exhibits a potent antitumor activity against MDA-MB-231 cells[1].
Anticancer agent 42 (10 μM, 24 h) induces G2 and S phase arrest in MDA-MB-231 cells[1].
Anticancer agent 42 (10 μM, 24 h) induces cell apoptosis by regulating the expression of apoptosis related proteins in MDA-MB-231 cells[1].
Anticancer agent 42 (0-1 μM) depolarizes mitochondrial membrane and decreases the mitochondrial membrane potential leading to apoptosis[1].
Anticancer agent 42 (0-1 μM, 24 h) induces the cells to produce a large amount of ROS[1].

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

Anticancer agent 42 相关抗体:

Cell Viability Assay

Cell Line: A549, MDA-MB-231, HeLa[1]
Concentration: 0-20 μM
Incubation Time: 4 h
Result: Exhibited a potent activity against MDA-MB-231 with an IC50 of 0.07 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 10 μM
Incubation Time: 24 h
Result: Induced G2 and S phase arrest in MDA-MB-231 cells; caused the percentage of MDA-MB-231 cells in G1 phase to decrease significantly (from 74.44% to 16.48%), cells in G1 phase to increase (from 16.61% to 28.47%), and in G2 phase to significantly increase (from 8.95% to 55.05%).

Apoptosis Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 10 μM
Incubation Time: 24 h
Result: Induced cell apoptosis, with apoptotic rate of 31.69%.

Western Blot Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 100 nM
Incubation Time: 48 h
Result: Increased the level of human apoptosis-related proteins (pro-caspase 3, catalase, HTRA2/Omi and p53) in MDA-MB-231 cell.

Western Blot Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 0.035, 0.07, 0.14, 0.21 μM
Incubation Time: 24 h
Result: Increased caspase 9, caspase3, cytochrome C and Bax expression, but decreased Bal-2 expression with increasing concentration.
体内研究
(In Vivo)

Anticancer agent 42 (compound 10d) (Kunming mice, 5000 mg/kg, Intragastric administration, once) has extremely low oral toxicity[1].
Anticancer agent 42 (Kunming mice, 238-600 mg/kg, IP, once) shows no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg[1].
Anticancer agent 42 (Kunming mice, 25 mg/kg, IP, once every two days) causes mild liver and kidney damage[1].
Anticancer agent 42 (BALB/c mice, suppresses breast cancer 4T1 tumor growth, the anti-tumor effect is better combined use with CA (Cyanoacrylates), and can cross through the skin to achieve anti-tumor effects.[1].

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

Animal Model: Kunming mice (n=10, 5 male and 5 female)[1]
Dosage: 5000 mg/kg
Administration: Intragastric administration, once
Result: Had extremely low oral toxicity, did not cause death in mice at 5000 mg/kg.
Animal Model: Kunming mice[1]
Dosage: 600, 476, 378, 300, 238 mg/kg
Administration: IP, once
Result: Showed no obvious liver and kidney damage to mice, with an LD50 of 374 mg/kg.
Animal Model: Kunming mice (n=3)[1]
Dosage: 25 mg/kg
Administration: IP, once every two days
Result: Caused mild liver and kidney damage after administration, slightly increased ALT, AST and BUN of mice.
Animal Model: BALB/c mice (4T1 tumor-bearing, female, eight groups, 6 mice per group)[1]
Dosage: 10d (50 mg/kg) + CA; 10d (50 mg/kg) + saline; 10d (200 mg/kg) + CA
Administration: Intratumoral injection, every four days (50 mg/kg); smear, every two days (200 mg/kg), for 14 days.
Result: Showed obvious antitumor effect from the 8th day; had protective effects on the spleens of tumor-bearing mice; the anti-tumor effect is better when combined use with CA; can cross through the skin to achieve anti-tumor effects.
分子量

391.25

Formula

C19H16Cl2N2O3
CAS 号
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

Anticancer agent 42 相关分类

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  • 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.

Keywords:

Anticancer agent 422687265-18-3Anticancer agent42Anticancer agent-42MDM-2/p53ApoptosisReactive Oxygen SpeciesMDA-MB-231 cellsAnti-breast cancer4T1 tumorAntitumor activityLow toxicityOrally activeInhibitorinhibitorinhibit

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