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25mg |
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FGFR1/DDR2 inhibitor 1 (compound 11k) is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
Targets |
DDR2 (IC50 = 3.2 nM); FGFR1 (IC50 = 31.1 nM)
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ln Vitro |
FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) significantly reduces FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. In H2286 cells, FGFR1/DDR2 inhibitor 1 significantly inhibits DDR2 phosphorylation in a dose-dependent manner over a 2-hour period (60-250 μM)[1].
FGFR1/DDR2 inhibitor 1 has IC50s of 108.4, 93.4, 31.8, and 306.6 nM against KG-1, SNU-16, NCI-H716, and UMUC14, respectively, which significantly inhibit the proliferation of FGFR-driven cancer cell lines. Significant activity is shown by FGFR1/DDR2 inhibitor 1 against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM)[1]. |
ln Vivo |
FGFR1/DDR2 inhibitor 1 (10–20 mg/kg; p.o.; once daily for 7 days) exhibits significant anti-tumor efficacy in the NCI-H1581 tumor model[1].
FGFR1/DDR2 inhibitor 1 was administered to randomized SCID mice with NCI-H2286 tumors at a dose of 10 mg/kg for ten days in a row. Tumor growth inhibition rates (TGI) of 82.8% were observed when FGFR1/DDR2 inhibitor 1 was used to inhibit tumor growth[1]. |
Animal Protocol |
Nude mice bearing NCI-H1581 tumors
10 or 20 mg/kg P.o.; once daily for 7 days |
References |
Molecular Formula |
C28H22F3N5O
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Molecular Weight |
501.50239610672
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Exact Mass |
501.18
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Elemental Analysis |
C, 67.06; H, 4.42; F, 11.36; N, 13.96; O, 3.19
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CAS # |
2308497-58-5
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Related CAS # |
2308497-58-5
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Appearance |
Solid powder
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SMILES |
CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=C(C=C3)C(=NN4)C5=CN(N=C5)C6CC6
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InChi Key |
ZEOWTGPWHLSLOG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H22F3N5O/c1-16-5-6-18(27(37)33-21-4-2-3-20(13-21)28(29,30)31)11-24(16)17-7-10-23-25(12-17)34-35-26(23)19-14-32-36(15-19)22-8-9-22/h2-7,10-15,22H,8-9H2,1H3,(H,33,37)(H,34,35)
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Chemical Name |
3-[3-(1-cyclopropylpyrazol-4-yl)-1H-indazol-6-yl]-4-methyl-N-[3-(trifluoromethyl)phenyl]benzamide
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Synonyms |
ZUN 97585; ZUN-97585; ZUN97585
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 100~250 mg/mL (199.4~498.5 mM)
Ethanol: ~100 mg/mL (~199.4 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.15 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9940 mL | 9.9701 mL | 19.9402 mL | |
5 mM | 0.3988 mL | 1.9940 mL | 3.9880 mL | |
10 mM | 0.1994 mL | 0.9970 mL | 1.9940 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.