Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. |
In vitro | EGFR/HER2-IN-7 (compound 39) demonstrates significant broad-spectrum cytotoxic efficacy, notably achieving an IC 50 value of 1.83 μM against MCF-7 breast cancer cell lines, indicating its potent anti-cancer capabilities [1]. This compound effectively induces apoptosis and cell cycle arrest at the G1/S phase within various cancer cell lines, including HepG2 hepatocellular carcinoma, MCF-7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, and HeLa cervical epithelioid carcinoma, upon exposure to concentrations ranging from 0-1 mM over 72 hours. Specifically, EGFR/HER2-IN-7 inhibits EGFR/HER2 kinase and DHFR activities; DHFR inhibition leads to S phase arrest, whereas EGFR/HER2 kinase inhibition results in G1 phase arrest. The compound also significantly hampers cancer cell growth, inducing apoptosis across the tested cell lines with IC 50 values of 3.48 μM (HepG2), 1.83 μM (MCF-7), 6.08 μM (HCT-116), 12.74 μM (PC-3), and 4.78 μM (HeLa), respectively, underscoring its potential as a versatile therapeutic agent in oncology [1]. |
In vivo | Caspase-3, a lysosomal enzyme pivotal for apoptosis, serves as a crucial biomarker for identifying apoptotic cells. Compound EGFR/HER2-IN-7, administered at a dosage of 10 mg/kg via intraperitoneal injection to Swiss albino female mice bearing breast cancer without lactating mammary glands, demonstrated significant anti-breast cancer efficacy over a duration of 20 days. The treatment not only reduced tumor volume by 76.5% and body weight by 17.4% but also notably increased Caspase-3 immunoexpression, with a Caspase-3 score of 1.33, underscoring its potential as a therapeutic agent against breast cancer. |
Molecular Weight | 379.23 |
Formula | C14H11BrN4O2S |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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EGFR/HER2/DHFR-IN-1 inhibitor inhibit