TYRA-200 free base · Synonyms: TYRA 200 · TYRA200

TYRA-200 is a potent and orally active FGFR2 inhibitor.

For research use only. Not for human or veterinary use.

Target FGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

TYRA-200 structure

CAS No.: 2823289-77-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 625.00	BP-02058-25mg	In stock	Get quote
50 mg	USD 985.00	BP-02058-50mg	In stock	Get quote
100 mg	USD 1,350.00	BP-02058-100mg	In stock	Get quote
250 mg	USD 1,920.00	BP-02058-250mg	In stock	Get quote
500 mg	Inquire	BP-02058-500mg	In stock	Inquire
1 g	Inquire	BP-02058-1g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer.

Biological activity

In Vitro TYRA-200 potently inhibits the enzymatic activity of FGFR2 gatekeeper mutants (V565L, V565F) and molecular brake mutants (N550D, N550H, N550K, E566A), and exhibits potent cellular growth inhibitory activity against Ba/F3 cells expressing FGFR2 variants N550K, V565F, V565I, K660E, and K660N. TYRA-200 maintains in vitro activity in AN3CA endometrial cancer cells harboring the FGFR2 N550K molecular brake mutation. In Vivo TYRA-200 induces 80% tumor regression in the AN3CA endometrial cancer xenograft model with the FGFR2 N550K molecular brake mutation, and 64% tumor regression in the Ba/F3 FGFR2 V565F allograft model with the FGFR2 V565F gatekeeper resistance mutation.

Identifiers

SMILES: C=CC(NC1=CC2=C(N(C=C2C)C3=C(C=NC(NC4=CN(N=C4)CC(C)(O)C)=N3)F)C=C1)=O
InChIKey: IMSVRBNZOZXJLS-UHFFFAOYSA-N

Specifications

MW (average): 449.4808
Formula: C₂₃H₂₄FN₇O₂
CAS No.: 2823289-77-4
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years; In solvent -20°C, 1 month.

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[1]. Rodon Ahnert J, et al. A multicenter, open-label, first-in-human study of TYRA-200 in advanced intrahepatic cholangiocarcinoma and other solid tumors with activating FGFR2 gene alterations (SURF201). J Clin Oncol. 2025;43(4 suppl):TPS646. doi: 10.1200/JCO.2025.43.4.suppl.TPS646

[2]. Allen E, et al. TYRA-200: Potent Against FGFR2 Fusions, Molecular Brake Mutations and Gatekeeper Resistance. Eur J Cancer. 2022;174 Suppl 1:S16.

Same target

Search FGFR

Same research area

Search Cancer