AZD4547 Inhibitor CAS No. 1035270-39-3

Cat. No.	Name	Size	Price
KI0595	AZD4547	5 mg	$176
	AZD4547	10 mg	$272
	AZD4547	50 mg	$912
	AZD4547	100 mg	$1392
	AZD4547	200 mg	$2032

Chemical Characteristic

Product Name	AZD4547
CAS No.	1035270-39-3
Molecular Weight	463.57
Formula	C₂₆H₃₃N₅O₃
Chemical Name	rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
Smiles	C(=O)(c1ccc(cc1)N1C[C@H](N[C@H](C1)C)C)Nc1n[nH]c(c1)CCc1cc(cc(c1)OC)OC
Chemical Structure
Documents	COA HPLC MS

Biological activities

AZD4547 is a potent selective FGFR inhibitor. The IC50s of AZD4547 against FGFR1, FGFR2, FGFR3 and FGFR4 are 0.2 , 2.5, 1.8 and 165 nM, respectively. AZD4547 also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC50 of 24 nM. In vitro, AZD4547 potently inhibits the proliferation of tumor cell lines KG1a, Sum52-PE and KMS11 with IC50 values of 18, 41, and 281 nM, respectively. AZD4547 potently inhibits FGFR phosphorylation and downstream signaling in human tumor cell lines KG1a, Sum52-PE and KMS11.^[1] The GI50 values of AZD4547 are 3 and 5 nM against gastric cancer cell lines SNU-16 and KATOIII (carrying the amplified FGFR2 gene), respectively. AZD4547 also effectively induces apoptosis in SNU-16 cells. In vivo, AZD4547 administration results in significant dose-dependent tumor growth inhibition in FGFR2-amplified xenograft (SNU-16) and patient-derived gastric cancer xenograft (PDGCX) models (SGC083), but not in non-amplified models.^[2] Furthermore, AZD4547 treatment also induces potent tumor stasis or regressive effects in four of five FGFR1-amplified squamous NSCLC patient-derived tumor xenograft (PDTX) models.^[3] In a representative FGFR-driven human tumor xenograft model, oral administration of AZD4547 (6.25 and 12.5 mg/kg) is well tolerated and results in potent dose-dependent antitumor activity, consistent with plasma exposure and pharmacodynamic modulation of tumor FGFR.^[1]

Protocols

In vivo: AZD4547 is formulated in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water. ^[1]

References

[1] Gavine PR, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012, 72(8): 2045-2056. [2] Xie L, et al. FGFR2 Gene Amplification in Gastric Cancer Predicts Sensitivity to the Selective FGFR Inhibitor AZD4547. Clin Cancer Res. 2013. [3] Zhang J, et al. Translating the therapeutic potential of AZD4547 in FGFR1-amplified non-small cell lung cancer through the use of patient-derived tumor xenograft models. Clin Cancer Res. 2012,18(24): 6658-6667.

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