6-bromo-2,8-dimethylimidazo[1,2-a]pyrazine cas 1845754-40-6

· Name: TTC-352
· CAS Number: 1845754-40-6
· Chemical Name: (E)-1-(4-(2-(4-cyclopropylpiperazin-1-yl)ethoxy)phenyl)-2-(4-hydroxyphenyl)-3-phenylprop-2-en-1-one
· Status: A selective estrogen receptor partial agonist, which was once a clinical candidate drug used for the treatment of advanced and metastatic breast cancer.
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Detailed Introduction
Background and Mechanism of Action
TTC-352 belongs to a class of drugs known as "selective estrogen receptor partial agonists". To understand its function, one needs to first grasp a classic target in breast cancer treatment - the estrogen receptor.
· Estrogen and Breast Cancer: Approximately 70% of breast cancers are "estrogen receptor positive", meaning that the growth of cancer cells depends on the binding of estrogen and estrogen receptors. Blocking this signaling pathway is the key to treatment.
· Existing Drugs and Their Limitations: Tamoxifen is the most well-known drug among them. It binds to estrogen receptors and prevents the effect of estrogen. However, long-term use of tamoxifen can cause conformational changes in the receptors, transforming them from antagonists to partial agonists, which may stimulate cancer cell growth and lead to drug resistance.
· The Innovation of TTC-352: TTC-352 is designed to address the problem of tamoxifen resistance. It also binds to estrogen receptors, but its unique chemical structure enables it to function as a more potent partial agonist. In cancer cells, this "super agonist" signal actually triggers cell apoptosis, or programmed cell death. Therefore, it has little effect on normal tissues, but can effectively kill breast cancer cells that have developed resistance to tamoxifen.
In simple terms, its mechanism is "fighting with poison": by overactivating the already "dysfunctional" estrogen receptor pathway, it induces the cancer cells to commit suicide.
2. Physical and Chemical Properties
· Molecular formula: C₃₀H₃₂N₂O₃
· Molecular weight: 468.59 g/mol
· Appearance: Usually a white to off-white solid powder.
3. Research and Clinical Status
· Research institution: TTC-352 was discovered and developed by the research team from the University of Illinois at Urbana-Champaign in the United States.
· Preclinical research: In the preclinical laboratory studies and animal models, TTC-352 demonstrated strong inhibitory activity against tamoxifen-resistant breast cancer cells and tumors.
· Clinical trials: TTC-352 has entered the Phase I clinical trial stage. The main purpose of this stage is to assess the safety, tolerability, pharmacokinetics of the drug in the human body and determine the appropriate dosage.
· Current status: According to public information, the clinical development of TTC-352 seems to have been suspended or terminated. This is very common in new drug development, and the reasons may include:
· Unexpected toxicity or side effects occurred during clinical trials.
· The efficacy did not reach the expected target.
· Strategic adjustments in the business plan, resources being allocated to more promising candidate drugs.
· Although its development may have stopped, as a representative of a new type of SERM, its research data and experience still have significant value for the development of other similar drugs.
4. Main Applications and Significance
· Main indications: It is intended for the treatment of advanced or metastatic hormone receptor-positive breast cancer that has developed resistance to tamoxifen or other endocrine therapies.
· Scientific significance: TTC-352 is an important practical and validation of the "selective estrogen receptor modulator" drug design concept. It demonstrates the feasibility of overcoming existing drug resistance by designing molecules with a specific efficacy spectrum (strong partial agonist).
Summary

CAS 1845754-40-6 (TTC-352) is a breast cancer candidate drug with an innovative mechanism of action. It represents a new strategy to overcome tamoxifen resistance, which involves inducing apoptosis in cancer cells through a potent partial agonistic effect. Although its own clinical development may have been halted, it provides valuable scientific insights and directions for the development of anti-cancer drugs, particularly in the field of endocrine therapy.