WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H204550
CAS#: 1035270-39-3
Description: AZD4547 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival.
Hodoodo Cat#: H204550
Name: AZD-4547
CAS#: 1035270-39-3
Chemical Formula: C26H33N5O3
Exact Mass: 463.26
Molecular Weight: 463.572
Elemental Analysis: C, 67.36; H, 7.18; N, 15.11; O, 10.35
Related CAS #: 1035270-39-3 1394854-62-6
Synonym: AZD4547; AZD-4547; AZD 4547, fexagratinib
IUPAC/Chemical Name: N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide
InChi Key: VRQMAABPASPXMW-HDICACEKSA-N
InChi Code: InChI=1S/C26H33N5O3/c1-17-15-31(16-18(2)27-17)22-9-6-20(7-10-22)26(32)28-25-13-21(29-30-25)8-5-19-11-23(33-3)14-24(12-19)34-4/h6-7,9-14,17-18,27H,5,8,15-16H2,1-4H3,(H2,28,29,30,32)/t17-,18+
SMILES Code: O=C(NC1=NNC(CCC2=CC(OC)=CC(OC)=C2)=C1)C3=CC=C(N4C[C@H](C)N[C@H](C)C4)C=C3
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Related CAS# Sci-Finder listed CAS#1394854-62-6 for AZD-4547 ChemIDplus listed CAS#1035270-39-3 for AZD-4547, see website: https://chem.nlm.nih.gov/chemidplus/rn/1035270-39-3 According to Sci-Finder, Chemical name for CAS#1394854-62-6: N-[3-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl]-4-(3,5-dimethyl-1-piperazinyl)benzamide Chemical name for CAS#1035270-39-3: rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
| Biological target: | AZD4547 inhibits FGFR1, FGFR2, FGFR3, and FGFR4 with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM, respectively. |
| In vitro activity: | AZD-4547 inhibited CRC (colorectal cancer) cell growth in vitro, and its activity correlated with the FGFR-1/2 expression level. AZD-4547 was cytotoxic and pro-apoptotic in FGFR-1/2-expressed CRC cell lines (NCI-H716 and HCT-116), but not in FGFR-1/2 null HT-29 cells. Further, AZD-4547 inhibited cell cycle progression and attenuated the activation of FGFR1-FGFR substrate 2 (FRS-2), ERK/mitogen-activated protein kinase (MAPK), and AKT/mammalian target of rapamycin (AKT/mTOR) signalings in NCI-H716 and HCT-116 cells. Reference: Tumour Biol. 2015 Jul;36(7):5641-8. https://link.springer.com/article/10.1007/s13277-015-3237-1 |
| In vivo activity: | To investigate the therapeutic potential of AZD4547, MMTV-ErbB2 mice with palpable spontaneous tumors were treated with AZD4547 (6 mg/kg/day) for 3 weeks. AZD4547 markedly repressed the TIC (tumor initiating cells) population in spontaneous tumors, as measured by the percent of ALDH+ tumor cells (Fig. 7a). Likewise, the self-renewal capacity and anchorage-independent growth of these tumor cells were significantly reduced in primary tumorsphere and 3D culture assays, respectively (Fig. 7b,c). Altogether, the stem cell data suggest that AZD4547 selectively targets (cancer stem cell) CSC/TIC populations, thus indicating a mechanism for the anti-cancer potential of AZD4547. Reference: Sci Rep. 2017 Sep 12;7(1):11306. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5595825/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 25.0 | 53.93 | |
| DMSO | 47.7 | 102.83 | |
| DMSO:PBS (pH 7.2) (1:1) | 0.5 | 1.08 | |
| Ethanol | 1.6 | 3.45 |
The following data is based on the product molecular weight 463.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Yao TJ, Zhu JH, Peng DF, Cui Z, Zhang C, Lu PH. AZD-4547 exerts potent cytostatic and cytotoxic activities against fibroblast growth factor receptor (FGFR)-expressing colorectal cancer cells. Tumour Biol. 2015 Jul;36(7):5641-8. doi: 10.1007/s13277-015-3237-1. Epub 2015 Feb 19. PMID: 25691251. 2. Zhao Q, Parris AB, Howard EW, Zhao M, Ma Z, Guo Z, Xing Y, Yang X. FGFR inhibitor, AZD4547, impedes the stemness of mammary epithelial cells in the premalignant tissues of MMTV-ErbB2 transgenic mice. Sci Rep. 2017 Sep 12;7(1):11306. doi: 10.1038/s41598-017-11751-7. PMID: 28900173; PMCID: PMC5595825. 3. Huang Y, Wang F, Li H, Xu S, Xu W, Pan X, Hu Y, Mao L, Qian S, Pan J. Inhibition of Fibroblast Growth Factor Receptor by AZD4547 Protects Against Inflammation in Septic Mice. Inflammation. 2019 Dec;42(6):1957-1967. doi: 10.1007/s10753-019-01056-4. PMID: 31321583. |
| In vitro protocol: | 1. Yao TJ, Zhu JH, Peng DF, Cui Z, Zhang C, Lu PH. AZD-4547 exerts potent cytostatic and cytotoxic activities against fibroblast growth factor receptor (FGFR)-expressing colorectal cancer cells. Tumour Biol. 2015 Jul;36(7):5641-8. doi: 10.1007/s13277-015-3237-1. Epub 2015 Feb 19. PMID: 25691251. 2. Zhao Q, Parris AB, Howard EW, Zhao M, Ma Z, Guo Z, Xing Y, Yang X. FGFR inhibitor, AZD4547, impedes the stemness of mammary epithelial cells in the premalignant tissues of MMTV-ErbB2 transgenic mice. Sci Rep. 2017 Sep 12;7(1):11306. doi: 10.1038/s41598-017-11751-7. PMID: 28900173; PMCID: PMC5595825. |
| In vivo protocol: | 1. Huang Y, Wang F, Li H, Xu S, Xu W, Pan X, Hu Y, Mao L, Qian S, Pan J. Inhibition of Fibroblast Growth Factor Receptor by AZD4547 Protects Against Inflammation in Septic Mice. Inflammation. 2019 Dec;42(6):1957-1967. doi: 10.1007/s10753-019-01056-4. PMID: 31321583. 2. Zhao Q, Parris AB, Howard EW, Zhao M, Ma Z, Guo Z, Xing Y, Yang X. FGFR inhibitor, AZD4547, impedes the stemness of mammary epithelial cells in the premalignant tissues of MMTV-ErbB2 transgenic mice. Sci Rep. 2017 Sep 12;7(1):11306. doi: 10.1038/s41598-017-11751-7. PMID: 28900173; PMCID: PMC5595825. |
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