1035270-39-3
AZD-4547
CAS: 1035270-39-3
Molecular Formula: C26H33N5O3
1035270-39-3 - Names and Identifiers
1035270-39-3 - Physico-chemical Properties
| Molecular Formula | C26H33N5O3 |
| Molar Mass | 463.57 |
| Density | 1.189 |
| Melting Point | 168-170°C |
| Boling Point | 621.7±55.0 °C(Predicted) |
| Solubility | DMSO 92 mg/mL (198.45 mM);Water <1 mg/mL (<1 mM);Ethanol <1 mg/mL (<1 mM); |
| Appearance | Form Solid, color Pale Yellow to Light Beige |
| pKa | 酸度系数(pKa) 13.66±0.10(Predicted) |
| Storage Condition | Refrigerator |
| Physical and Chemical Properties | Bioactive AZD4547 (ABSK 091) is a new selective FGFR inhibitor, which targets FGFR1/2/3. In cell-free test, IC50 is 0.2 nM/2.5 nM/1.8 nM, which has weak activity on FGFR4, VEGFR2(KDR) and almost no activity on IGFR, CDK2 and p38. Phase 2/3. |
| Use | A novel selective FGFR inhibitor targeting FGFR1, FGFR2, and FGFR3. |
1035270-39-3 - Introduction
AZD4547 is a new selective FGFR inhibitor, targeting FGFR1/2/3,IC50 is 0.2 nM/2.5 nM/1.8 nM, has weak activity on FGFR4, VEGFR2(KDR), and almost no activity on IGFR, CDK2 and p38. Phase 2/3.
Last Update：2022-10-16 17:30:58
1035270-39-3 - Uses and synthesis methods
in vitro studies
Compared with FGFR1-3, AZD4547 acts on FGFR4 with weak activity, IC50 is 165 nM. AZD4547 only inhibits the activity of recombinant VEGFR2 (KDR) kinase with IC50 of 24 nM and selectively acts on a group of representative human kinases in vitro. 0.1 μM AZD4547 acts on a series of recombinant kinases, including ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2, and PI3K, with no activity. Accordingly, in cell phosphorylation experiments, it can be observed that the selectivity of AZD4547 acting on FGFR1-3 is higher than that of FGFR4, IGFR, and KDR. AZD4547 In vitro, only tumor cells that express to regulate FGFRs such as KG1a, Sum52-PE, and KMS11 have effective antiproliferative activity with IC50 of 18-281 nM, but are inactive to MCF7 and more than 100 other tumor cells. AZD4547 treatment of human tumor cells effectively inhibits FGFR and MAPK phosphorylation, which is dose-dependent. AZD4547 also effectively inhibit FRS2 and PLC & gamma; Phosphorylation, and downstream FGFR signal. In addition, AZD4547 acts on breast cell lines, MCF7 and Sum52-PE instead of KG1a and KMS11 cells, affecting AKT phosphorylation. AZD4547 treatment of Sum52-PE and KMS11 cells significantly induced apoptosis, acting on KG1a cells, significantly improving cell cycle arrest in G1 phase instead of apoptosis, while acting on MCF7 cells had no effect on cell cycle distribution and apoptosis.
In vivo studies
AZD4547 the mice carrying KMS11 tumor were treated orally at a dose of 3 mg/kg twice a day. Compared with the blank control group, the growth of 53% tumor was significantly inhibited. AZD4547 the mice were treated at a dose of 12.5 mg/kg once a day or 6.25 mg/kg twice a day, the tumor was completely inhibited, which was positively correlated with the pharmacodynamic regulation dose of p-FGFR3 and reduced the proliferation of KMS11 tumor cells. Moreover, FGFR1 was AZD4547 administered orally at a dose of 12.5 mg/kg to fuse KG1a transplanted tumor model once a day to inhibit 65% tumor growth. At the effective dose level, AZD4547 did not show an anti-angiogenic effect. AZD4547 has no significant effect on blood pressure, so it lacks anti-KDR activity in vivo. Correspondingly, Cediranib-sensitive transplanted tumor models, including Calu-6, HCT-15 and LoVo, were AZD4547 treated orally at a dose of 6.25 mg/kg twice daily with no activity.
Last Update：2024-04-09 21:01:54
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Product Name: AZD4547 Visit Supplier Webpage Request for quotationCAS: 1035270-39-3
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Mobile: 18021002903
QQ: 3008007409
Multiple SpecificationsSpot supply
Product Name: AZD4547; ADSK091 Visit Supplier Webpage Request for quotationCAS: 1035270-39-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: AZD4547 Visit Supplier Webpage Request for quotationCAS: 1035270-39-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: AZD4547 Visit Supplier Webpage Request for quotationCAS: 1035270-39-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: AZD4547 Visit Supplier Webpage Request for quotationCAS: 1035270-39-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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