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TYRA-300 CAS 2800223-30-5 Product Introduction

TYRA-300, also named Dabogratinib, is a potent and highly selective oral FGFR3 inhibitor. It is an investigational compound targeting FGFR3-related malignant tumors and skeletal diseases, with low off-target effect on other FGFR subtypes.

Basic Chemical Information

CAS Number: 2800223-30-5

Molecular Formula: C₂₅H₂₄Cl₂N ₆ O₃S

Molecular Weight: 559.47 g/mol

Common Purity: Not less than 98%

Appearance: Off-white to pale yellow crystalline solid

Solubility: Dissolvable in DMSO, methanol and ethanol, slightly soluble in water

Storage Condition: Store powder at -20 ℃ , stock solution at -80 ℃

Action Mechanism

Its main acting target is fibroblast growth factor receptor 3. It binds with FGFR3 kinase domain in ATP competitive reversible way, blocks downstream signal transmission, and restrains proliferation of tumor cells.

It presents high selectivity to FGFR3, with obvious weaker inhibitory effect on FGFR1, FGFR2 and FGFR4, effectively reducing adverse reactions caused by non-specific inhibition. The IC50 value in targeted cells is 11 nM, showing strong pharmacological activity.

Application Scope

Tumor treatment

It is mainly applied to research and clinical research of urothelial carcinoma. FGFR3 gene variation is common in bladder cancer lesions. The product can inhibit lesion development, and relevant clinical trials are underway for recurrent and advanced solid tumors.

Skeletal disorder research

It is used for research treatment of achondroplasia. Pathogenic mutation of FGFR3 will hinder bone growth, and this compound can improve chondrocyte growth status and adjust skeletal development.

Product Characteristics

It has good oral absorption property, suitable for daily oral administration. It works for multiple common FGFR3 mutation types and drug-resistant variants. Products are divided into research grade and clinical grade, meeting different experimental and trial usage demands.

Usage Notice

This product is only for laboratory research use, not applicable to human body and animal clinical medication.

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