Derazantinib hydrochloride salt form · hydrochloride · Parent ARQ-087 · Synonyms: ARQ 087 2HCl | AQ 14741087 | Derazantinib dihydrochloride
Derazantinib dihydrochloride is an ATP competitive and orally activeFGFR inhibitor.
For research use only. Not for human or veterinary use.
Purity >98%
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Description
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models.
Identifiers
- SMILES
-
FC1=C([C@H]2C=3C(C=4C(C2)=CN=C(NC5=CC(CCNCCOC)=CC=C5)N4)=CC=CC3)C=CC=C1.Cl - InChIKey
-
FJQGYPSAODOLEW-UFTMZEDQSA-N
Specifications
- MW (average)
- 505.0260
- Formula
- C29H30ClFN4O
- CAS No.
- 1821329-75-2
- 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 -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
Documents
References
[1]. Hall TG, et al. Preclinical Activity of ARQ-087, a Novel Inhibitor Targeting FGFR Dysregulation. PLoS One. 2016 Sep 14;11(9):e0162594.
[2]. Balek L, et al. ARQ-087 inhibits FGFR signaling and rescues aberrant cell proliferation and differentiation in experimental models of craniosynostoses and chondrodysplasias caused by activating mutations in FGFR1, FGFR2 and FGFR3. Bone. 2017 Dec;105:57-66.
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