Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.
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- CAS No.: 2800223-30-5
- Formula: C25H24Cl2N6O3S
- Molecular Weight:559.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR3 11 nM (IC50) |
FGFR2 157 nM (IC50) |
FGFR1 278 nM (IC50) |
FGFR4 405 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DMS-114 | IC50 |
205 nM
Compound: 22
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Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay
Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay
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[PMID: 39258897] |
| KG-1 | IC50 |
109 nM
Compound: 22
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Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
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[PMID: 39258897] |
| RT-4 | IC50 |
10 nM
Compound: 22
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Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
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[PMID: 39258897] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2800223-30-5
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Molecular Weight 559.47
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Formula C25H24Cl2N6O3S
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SMILES
O=S(N(C1)CC1(C2)CN2C(N=C3)=CC=C3C4=NNC5=CC=C(O[C@H](C)C6=C(Cl)C=NC=C6Cl)C=C54)(C)=O
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Synonyms
TYRA-300 (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Starrett JH, et al. Dabogratinib (TYRA-300), an FGFR3 isoform-selective inhibitor: preclinical and initial clinical evidence of anti-tumor activity. Mol Cancer Ther. Published online October 14, 2025. [Content Brief]
[2]. Starrett JH, et al. TYRA-300, an FGFR3-selective inhibitor, promotes bone growth in two FGFR3-driven models of chondrodysplasia. JCI Insight. 2025;10(9):e189307. Published 2025 Apr 3. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dabogratinib (GMP) Related Classifications
HY-159642G Related Classifications
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