TYRA-300 free base · Synonyms: TYRA 300 · TYRA300
TYRA-300 is an FGFR3-selective inhibitor agnostic to the gatekeeper mutation, with less hyperphosphatemia mediated by FGFR1 inhibition than pan-FGFR…
For research use only. Not for human or veterinary use.
TYRA-300 structure
CAS No.: 2800223-30-5
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 580.00 | BP-00906-100mg | In stock | Get quote |
| 250 mg | USD 928.00 | BP-00906-250mg | In stock | Get quote |
| 500 mg | USD 1,328.00 | BP-00906-500mg | In stock | Get quote |
| 1 g | Inquire | BP-00906-1g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
TYRA-300 is an FGFR3-selective inhibitor agnostic to the gatekeeper mutation, with less hyperphosphatemia mediated by FGFR1 inhibition than pan-FGFR inhibitors in preclinical models.
Biological activity
In Vitro Dabogratinib (0.046 nM-3 μM; 2 h) induces dose-dependent downregulation of the FGFR3 downstream signaling pathway (assessed by pERK1/2 levels) in RT112/84, RT112/84-V555M and UM-UC-14 bladder cancer cell lines. Dabogratinib inhibits the viability of FGFR3-driven bladder cancer cell lines, with IC50 values of 9 nM for the RT112/84 cell line, 17 nM for the RT112/84-V555M cell line, and 16 nM for the UM-UC-14 cell line. In Vivo Dabogratinib (3-18 mg/kg; p.o.; twice/once daily; 21 days) exhibits dose-dependent in vivo efficacy in urothelial carcinoma xenograft models harboring FGFR3S249C. Dabogratinib (12.5 mg/kg; p.o.; twice daily) induces tumor regression in FGFR3::TACC3 fusion urothelial carcinoma xenograft models and FGFR3V555M urothelial carcinoma xenograft models. Dabogratinib (8-14 mg/kg; p.o.; once daily; 4 weeks) dose-dependently increases the growth rate of wild-type mice and promotes their long bone growth in vivo. Dabogratinib (1.2 mg/kg; s.c.; once daily; 15 days) promotes bone growth, improves skeletal proportions, optimizes growth plate structure, and increases the foramen magnum size in the Fgfr3Y367C/+ mouse model of achondroplasia (ACH). Dabogratinib (1.8 mg/kg; s.c.; once daily; 21 days) increases bone length, enlarges foramen magnum size and improves intervertebral disc morphology in the Fgfr3N534K/+ mouse model of HCH.
Identifiers
- SMILES
-
C[C@@H](OC1=CC2=C(NN=C2C2=CC=C(N=C2)N2CC3(C2)CN(C3)S(C)(=O)=O)C=C1)C1=C(Cl)C=NC=C1Cl - InChIKey
-
JOAFWIHZEBKYQK-OAHLLOKOSA-N
Specifications
- MW (average)
- 559.4670
- Formula
- C25H24Cl2N6O3S
- CAS No.
- 2800223-30-5
- Physical state
- Solid
- Color
- white to off-white
- 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 4℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO