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Shanghai Chaolan Chemical Technology Center
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| Products Intro: |
Product Name:ZUN97585,FGFR1/DDR2 inhibitor 1
CAS:2308497-58-5
Purity:98% Package:5MG;10MG;50MG;100MG,1G,5G,100G
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| | FGFR1/DDR2 inhibitor 1 Basic information |
| Product Name: | FGFR1/DDR2 inhibitor 1 | | Synonyms: | FGFR1/DDR2 inhibitor 1;ZUN97585;ZUN97585(FGFR1/DDR2 inhibitor 1);Inhibitor,NCI-H1581,FGFR-1/DDR2 inhibitor 1,FGFR1/DDR2 inhibitor 1,NCI-H2286,inhibit,cells,Nude,phosphorylation,mice,Fibroblast growth factor receptor,Discoidin Domain Receptor,tumor,SCID,FGFR;Benzamide, 3-[3-(1-cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl]-4-methyl-N-[3-(trifluoromethyl)phenyl]-;3-(3-(1-Cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide | | CAS: | 2308497-58-5 | | MF: | C28H22F3N5O | | MW: | 501.5 | | EINECS: | | | Product Categories: | | | Mol File: | 2308497-58-5.mol |  |
| | FGFR1/DDR2 inhibitor 1 Chemical Properties |
| Boiling point | 649.9±55.0 °C(Predicted) | | density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (498.50 mM; Need ultrasonic) | | pka | 12.82±0.40(Predicted) |
| | FGFR1/DDR2 inhibitor 1 Usage And Synthesis |
| Biological Activity | FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity[1].
FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells[1]. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC50s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM)[1].
FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model[1].SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8%[1]. | | References | [1]. Wang Q, et al. Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. Eur J Med Chem. 2019 Feb 1;163:671-689. |
| | FGFR1/DDR2 inhibitor 1 Preparation Products And Raw materials |
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