FGFR1/DDR2 inhibitor 1
- Product Name
- FGFR1/DDR2 inhibitor 1
- CAS No.
- 2308497-58-5
- Chemical Name
- FGFR1/DDR2 inhibitor 1
- Synonyms
- ZUN97585;FGFR1/DDR2 inhibitor 1;ZUN97585(FGFR1/DDR2 inhibitor 1);FGFR1/DDR2 inhibitor 1, 10 mM in DMSO;3-(3-(1-Cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;Benzamide, 3-[3-(1-cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl]-4-methyl-N-[3-(trifluoromethyl)phenyl]-;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
- CBNumber
- CB28054401
- Molecular Formula
- C28H22F3N5O
- Formula Weight
- 501.5
- MOL File
- 2308497-58-5.mol
FGFR1/DDR2 inhibitor 1 Property
- 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)
- form
- Solid
- color
- Off-white to light yellow
N-Bromosuccinimide Price
- Product number
- CS-0082049
- Product name
- FGFR1/DDR2inhibitor1
- Purity
- 99.03%
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0082049
- Product name
- FGFR1/DDR2inhibitor1
- Purity
- 99.03%
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0082049
- Product name
- FGFR1/DDR2inhibitor1
- Purity
- 99.03%
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-0082049
- Product name
- FGFR1/DDR2inhibitor1
- Purity
- 99.03%
- Packaging
- 50mg
- Price
- $2200
- Updated
- 2021/12/16
- Product number
- CS-0082049
- Product name
- FGFR1/DDR2inhibitor1
- Purity
- 99.03%
- Packaging
- 100mg
- Price
- $3400
- Updated
- 2021/12/16
FGFR1/DDR2 inhibitor 1 Chemical Properties,Usage,Production
Uses
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].
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].
in vivo
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].
| Animal Model: | Nude mice bearing NCI-H1581 tumors[1] |
| Dosage: | 10 or 20 mg/kg |
| Administration: | P.o.; once daily for 7 days |
| Result: | Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively. |
IC 50
FGFR1: 31.1 nM (IC50); DDR2: 3.2 nM (IC50)
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
Raw materials
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