1. Apoptosis
  2. Apoptosis
  3. Apoptosis inducer 7

Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity.

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Apoptosis inducer 7 Chemical Structure

Apoptosis inducer 7 Chemical Structure

CAS No. : 2252278-57-0

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Description

Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity[1].

In Vitro

Apoptosis inducer 7 (Compound 5I) (0.098-50 μM, 96 hours; human tumor cell lines) exerts the most potent antitumor activities against human cancer cell lines[1].
Apoptosis inducer 7 (Compound 5I) induces apoptosis in HCT-116 cells, and the apoptosis induction is related to the downregulation of anti-apoptotic protein c-Flip and upregulation of pro-apoptotic protein Noxa[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: Human breast cancer MDA-MB-231 cells, human lung cancer A549 cells, human colorectal cancer HCT-116 cells, human liver cancer HepG-2 cells and one non-tumor human breast epithelial MCF-10A cells.
Concentration: 0.098-50 μM
Incubation Time: 96 hours
Result: Inhibited with IC50 values of 0.22, 0.15, 0.42, 0.14 and 1.03 μM for MDA-MB-231, A549, HCT-116, HepG-2 and MCF-10A, respectively.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 0.75 and 1.0 μM
Incubation Time: 24 hours
Result: More than 40% of the cells were detected in the sub G1 phase.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 0.75 and 1.0 μM
Incubation Time: 24 hours
Result: Induced cleavage of PARP, caspases and decreased the levels of c-Flip and HDAC3 proteins.
In Vivo

Apoptosis inducer 7 (Compound 5I) (5 mg/kg; i.p.; three times a week, for 14 days; LL/2 xenograft model in C57/ BL6J mice) inhibits tumor growth[1].

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

Animal Model: KARPAS-422 subcutaneous xenograft in mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; three times a week, for 14 days.
Result: Inhibited the tumor growth with an inhibition rate of 62.3%, without significant body weight loss.
Molecular Weight

797.07

Formula

C49H68N2O7

CAS No.
SMILES

C[C@]12[C@@](C(C=C3[C@]2(CC[C@@]4([C@@]3([H])C[C@](C)(CC4)C(OCC5=CC=CC=C5)=O)C)C)=O)([H])[C@@]6([C@@](C(C)(C(/C(C6)=C/C(NC7CCN(CC7)C(OC(C)(C)C)=O)=O)=O)C)([H])CC1)C

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    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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