AZD4547

Description

APIM050097: AZD4547

CAS No.: 1035270-39-3

IUPAC/Chemical Name: N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide

Molecular Formula: C₂₆H₃₃N₅O₃ . 0.2HCl . 0.4H₂O

Molecular Weight: 478.1

Purity: >99% purity (HPLC at 214 and 254 nm)

QC: HPLC, ¹HNMR and quantitative microanalysis

Solubility: In DMSO, water with 1 eq. of acid

Storage: Store at 0°C (short term), -20°C (long term), desiccated

Background Information:

AZD4547 is a potent selective inhibitor of the FGFR family with IC50 of 0.2nM, 2.5nM, 1.8nM, and 165nM, respectively, for FGFR1, FGFR2, FGFR3, and FGFR4 in cell-free assays.

In Vitro: AZD4547 also inhibits recombinant VEGFR2 (KDR) kinase activity (IC50 = 24nM). AZD4547 potently inhibits autophosphorylation of FGFR1, 2 and 3 tyrosine kinases (IC50 = 12, 2, 40nM, respectively). but weaker inhibition of FGFR4 cellular kinase activity (IC50 = 142nM) in KG1a, Sum52-PE, MCF7, and KMS11 cell lines. AZD4547 also inhibits FGFR phosphorylation and downstream signaling affected FRS2, PLC, and MAPK at the cellular level [1].

In Vivo: Female SCID Mice with KMS11 tomors are treated chronically with AZD4547, and shows dose-dependent tumor growth inhibition with oral AZD4547 treatment. Twice a day AZD4547 at 3 mg/kg shows significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test), and complete tumor stasis (P<0.0001) with doses of 12.5 mg/kg once per day and 6.25 mg/kg twice a day. KG1a model with 12.5 mg/kg once per day results in 65% tumor growth inhibition (P=0.002) [1].

Reference: [1]. Gavine, P. R.; Mooney, L.; Kilgour, E.; Thomas, A. P.; Al-Kadhimi, K.; Beck, S.; Rooney, C.; Coleman, T.; Baker, D.; Mellor, M. J.; Brooks, A. N.; Klinowska, T.; “AZD4547: An Orally Bioavailable, Potent, and Selective Inhibitor of the Fibroblast Growth Factor Receptor Tyrosine Kinase Family”, Cancer Res. 2012, 72, 2045-2056.

Questions and Answers:

Question: How to make AZD4547 stock solution?

Answer: (In Vitro) AZD4547 was prepared as a 10 mmol/L stock solution in DMSO (Need ultrasonic), and diluted in the relevant assay media [1]. (In Vivo) AZD4547 was formulated in a 1%(v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water [1]. Add each solvent one by one: 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline; solubility: ≥2.5 mg/mL (5.39 mM); clear solution.

Question: What are FGFR inhibitors?

Answer: Frequent tumor fibroblast growth factor receptor (FGFR) are seen in many cancers, and include genetic amplifications, mutations, rearrangements, and fusions. FGFR inhibitors target these receptor alterations and show promise as a drug class. So far, five distinct membrane FGFR have been identified in vertebrates and all of them belong to the tyrosine kinase superfamily (FGFR1, FGFR2, FGFR3, FGFR4, and FGFR6). Selective FGFR inhibitors include Ponatinib (AP24534), Sulfatinib (FGFR1); FIIN-2. Zoligratinib (Debio-1347) (FGFR1,2); Dovitinib (TKI-258), Dovitinib (TKI258) Lactate (FGFR1,3); Infigratinib (BGJ398), AZD4547, PRN1371, Pemigatinib (INCB054828) (FGFR 1,2,3); Futibatinib (TAS120), ASP5878, Derazantinib (ARQ-087), LY2874455 (FGFR1,2,3,4); and H3B-6527, Roblitinib (FGF401) (FGFR4).

Question: Do you ship your AZD4547 to Europe by DHL or FedEx?

Answer: Yes, normally FedEx and sometimes DHL if clients request.

 

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Additional information

Ship from Country	USA
Size	10 mg, 100 mg, 200 mg, 50 mg

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