PD153035 Hydrochloride (CAS: 183322-45-4) is a small molecule inhibitor of the epidermal growth factor receptor (EGFR), also known as ErbB1 or HER1. It is a potent and specific inhibitor that has been extensively studied in cancer research, particularly in the treatment of non-small cell lung cancer (NSCLC).
Chemical name: N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazolin-4-amine hydrochloride
Molecular formula: C21H21ClFN5O2.HCl
Formula weight: 485.34 g/mol
CAS No: 183322-45-4
Top ten keywords from Google and synonyms:
Synonyms: PD-153035 hydrochloride, AG1538, SU5271, ZD-1839
Health benefits of this product:
As an EGFR inhibitor, PD153035 Hydrochloride has shown promising anti-tumor activity in preclinical studies, particularly against NSCLC. It blocks the activation of EGFR, which is often overexpressed or mutated in cancer cells, leading to uncontrolled cell proliferation, survival, and invasion. By inhibiting EGFR signaling, PD153035 Hydrochloride can induce apoptosis (cell death) and sensitize cancer cells to chemotherapy or radiation therapy.
In addition to NSCLC, PD153035 Hydrochloride has also demonstrated efficacy against other types of cancer, such as breast cancer and head and neck cancer. Moreover, it may have potential therapeutic applications beyond cancer, such as in asthma, psoriasis, and Alzheimer's disease, as EGFR has been implicated in these conditions as well.
Potential effects:
The potential effects of PD153035 Hydrochloride depend on its target, EGFR, which is a key player in many cellular processes, including proliferation, differentiation, migration, and survival. By inhibiting EGFR, PD153035 Hydrochloride can modulate these processes and exert various effects on cells, such as:
Inducing apoptosis: Blocking EGFR can trigger programmed cell death, which is a natural mechanism for removing damaged or abnormal cells. Apoptosis is often impaired in cancer cells, leading to their uncontrolled growth and resistance to therapy. PD153035 Hydrochloride can overcome this resistance and enhance cancer cell killing.
Inhibiting proliferation: EGFR activation promotes cell division, and its inhibition can slow down or stop cell growth. This effect is particularly relevant in cancer, where rapid proliferation is a hallmark feature. PD153035 Hydrochloride can reduce tumor size and prevent metastasis by blocking EGFR-mediated signaling.
Sensitizing to therapy: EGFR inhibition can sensitize cancer cells to other treatments, such as chemotherapy or radiation therapy. By suppressing EGFR-dependent survival signals, PD153035 Hydrochloride can increase the susceptibility of cancer cells to these modalities and enhance their effectiveness.
Modulating immunity: EGFR is also involved in regulating immune responses, and its inhibition can affect the interaction between cancer cells and immune cells. PD153035 Hydrochloride may enhance the antitumor immune response and improve the efficacy of immunotherapy.
Product mechanism:
PD153035 Hydrochloride works by binding to the ATP-binding site of EGFR and preventing its autophosphorylation, which is necessary for its activation and downstream signaling. This action blocks the activation of multiple signaling pathways, such as MAPK, PI3K/Akt, and STAT, which are involved in cell growth, survival, and motility. By interfering with these pathways, PD153035 Hydrochloride can induce apoptosis and inhibit proliferation and invasion.
Safety:
Like any drug, PD153035 Hydrochloride has potential side effects and safety concerns that should be taken into account. Some of the reported adverse effects include gastrointestinal disturbances, skin rash, headache, and fatigue. In rare cases, severe allergic reactions or liver toxicity may occur. Moreover, since EGFR is also expressed in normal tissues, such as skin, hair follicles, and gut epithelium, EGFR inhibition may lead to adverse effects on these organs, such as skin rash, alopecia, and diarrhea.
Dosing information:
PD153035 Hydrochloride is typically administered orally or intravenously, depending on the formulation and indication. The optimal dose and duration of treatment may vary depending on the patient's condition, age,
