Description Features In vitro In vivo
ChemicalBook > CAS DataBase List > AZD-4547

AZD-4547

Description Features In vitro In vivo
Product Name
AZD-4547
CAS No.
1035270-39-3
Chemical Name
AZD-4547
Synonyms
CS-21;AZD-4547;13C6]-AZD4547;AZD4547, >=98%;AZD4547/AZD-4547;AZD4547, Free Base, >99%;AZD4547 FGFR inhibitor AZD-4547;AZD4547, 98%, a potent inhibitor of the FGFR family;N-(3-(3,5-dimethoxyphenethyl)-1H-pyrazol-5-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide;N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide
CBNumber
CB92546547
Molecular Formula
C26H33N5O3
Formula Weight
463.57
MOL File
1035270-39-3.mol
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AZD-4547 Property

Melting point:
168-170°C
Boiling point:
621.7±55.0 °C(Predicted)
Density 
1.189
storage temp. 
Refrigerator
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
13.66±0.10(Predicted)
form 
Solid
color 
Pale Yellow to Light Beige
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13111
Product name
AZD 4547
Purity
≥98%
Packaging
5mg
Price
$110
Updated
2024/03/01
Cayman Chemical
Product number
13111
Product name
AZD 4547
Purity
≥98%
Packaging
10mg
Price
$165
Updated
2024/03/01
Cayman Chemical
Product number
13111
Product name
AZD 4547
Purity
≥98%
Packaging
50mg
Price
$595
Updated
2024/03/01
Usbiological
Product number
474071
Product name
AZD 4547
Packaging
100mg
Price
$2272
Updated
2021/12/16
TRC
Product number
A808120
Product name
AZD4547
Packaging
100mg
Price
$150
Updated
2021/12/16
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AZD-4547 Chemical Properties,Usage,Production

Description

AZD4547 is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.

Features

Greater selectivity for FGFR1-3 over FGFR4. AZD4547 is active against the tyrosine kinase activity of both the wild-type and mutant forms of FGFR.

In vitro

Compared to FGFR1-3, AZD4547 displays weaker activity against FGFR4 with IC50 of 165 nM. AZD4547 only inhibits recombinant VEGFR2 (KDR) kinase activity with IC50 of 24 nM, in the in vitro selectivity test against a diverse panel of representative human kinases. AZD4547 at 0.1 μM exhibits no activity against a range of recombinant kinases including ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2, and PI3-kinase. Consistently, the potent selectivity of AZD4547 for FGFR1-3 over FGFR4, IGFR, and KDR is also observed in cellular phosphorylation assays. AZD4547 has potent in vitro antiproliferative activity only against tumor cell lines expressing deregulated FGFRs such as KG1a, Sum52-PE, and KMS11 with IC50 of 18-281 nM, and is inactive against MCF7 as well as more than 100 additional tumor cell lines. AZD4547 treatment potently inhibits FGFR and MAPK phosphorylation in human tumor cell lines in a dose-dependent manner. AZD4547 also potently inhibits the phosphorylation of FRS2 and PLCγ, downstream markers of FGFR signaling. Notably, AZD4547 affects the AKT phosphorylation in the breast cell lines, MCF7 and Sum52-PE but not in KG1a and KMS11 lines. AZD4547 treatment significantly induces apoptosis in Sum52-PE and KMS11 cells, dramatically increases G1 arrest but not apoptosis in KG1a cells, and has no effect on cell cycle distribution or apoptosis in MCF7 cells.

In vivo

Oral administration of AZD4547 at 3 mg/kg twice daily in mice bearing KMS11 tumors results in significant tumor growth inhibition of 53% when compared with vehicle-treated controls, and AZD4547 at 12.5 mg/kg once daily or 6.25 mg/kg twice daily leads to complete tumor stasis, which is associated with dose proportional pharmacodynamic modulation of phospho-FGFR3 and reduced KMS11 tumor cell proliferation. Moreover, oral administration of AZD4547 at 12.5 mg/kg once daily results in 65% tumor growth inhibition in the FGFR1-fusion KG1a xenograft model. At efficacious dose levels, AZD4547 does not exhibit antiangiogenic effects. AZD4547 has no significant effect on blood pressure and therefore lacks in vivo anti-KDR activity. Consistently, dosing of 6.25 mg/kg orally twice daily AZD4547 is inactive in the cediranib-sensitive xenograft models including Calu-6, HCT-15 and LoVo.

Description

AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC50 values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively. It displays weaker activity against FGFR4 (IC50 = 165 nM), VEGFR2 (IC50 = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC50 = 581 nM), cyclin-dependent kinase 2 (IC50 = >10 μM), and p38 (IC50 = >100 μM). AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM). In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.

Chemical Properties

Pale Yellow Solid

Uses

AZD4547 is a bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinases. AZD4547 is particularly effective in inhibiting FGFR1, 2, and 3 tyrosine k inases and is under clinical investigation for the treatment of FGFR-dependent tumors.

Definition

ChEBI: AZD4547 is a member of the class of benzamides that is a carboxamide resulting from the formal condensation of the carboxy group of 4-(cis-3,5-dimethylpiperazin-1-yl)benzoic acid with the amino substituent of 5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-amine. It is an inhibitor of the fibroblast growth factor receptor (FGFR). It has a role as a fibroblast growth factor receptor antagonist. It is a member of pyrazoles, a N-arylpiperazine and a member of benzamides.

target

FGFR1

storage

Store at -20°C

AZD-4547 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD-4547 Suppliers

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View Lastest Price from AZD-4547 manufacturers

Honest Joy Holdings Limited
Product
AZD-4547 1035270-39-3
Price
US $0.00/KG
Min. Order
1KG
Purity
97.4%
Supply Ability
100 tons
Release date
2022-01-13

1035270-39-3, AZD-4547Related Search:

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  • AZD-4547
  • rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
  • AZD4547/AZD-4547
  • AZD4547, Free Base, >99%
  • rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide AZD4547
  • N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-rel-3,5-dimethylpiperazin-1-yl)benzamide
  • rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide
  • AZD4547, >=98%
  • CS-21
  • N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide
  • rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benz
  • AZD-4547;REL-N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-3-YL]-4-[(3R,5S)-3,5-DIMETHYL-1-PIPERAZINYL]BENZAMIDE;AZD4547/AZD-4547;AZD4547, FREE BASE, >99%;REL-N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-3-YL]-4-[(3R,5S)-3,5-DIMETHYL-1-PIPERAZINYL]BENZ
  • N-(3-(3,5-dimethoxyphenethyl)-1H-pyrazol-5-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide
  • Benzamide, N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-, rel-
  • AZD4547, 98%, a potent inhibitor of the FGFR family
  • N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide
  • 13C6]-AZD4547
  • AZD4547 FGFR inhibitor AZD-4547
  • 1035270-39-3
  • C26H33N5O3
  • Inhibitors
  • Anti-cancer&immunity
  • API