Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
FGFR4WT 17.1 nM (IC50) FGFR3 29.6 nM (IC50) FGFR4V550L 30.7 nM (IC50) FGFR2 46.7 nM (IC50) FGFR1 64.3 nM (IC50)
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ln Vitro |
FGFR-IN-9(Compound 19)(0-2 mM; 72 h) suppresses the proliferation of Ba/F3 FGFR4WT and Ba/F3 FGFR4V550L cells with IC50s of 82.5 ± 19.2 nM and 82.5 nM, respectively, and inhibits HUH7 cells with an IC50 of 94.7±28.6 nM. 260.0 ± 50.2 nM was reported [1]. Inhibiting the FGFR signaling pathway, FGFR-IN-9 (0-400 nM; 4 h)[1].
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ln Vivo |
Compound 19 (FGFR-IN-9) In the HUH7 xenograft mouse model, (30 and 45 mg/kg; ir; daily for 3 weeks) has anti-tumor efficacy [1]. FGFR-IN-9 (Compound 19) In Vivo Pharmacokinetic Profile Information [1] T1/2 (h) FGFR-IN-9 iv 1 mg/kg po 10 mg/kg 1.75 965 AUCINF (h·ng/mL) 177 1087 MRTinf (h) 1.3 2.37 Tmax (h) / 2 Cmax (ng /mL) / 202 AUCmax (h·ng/mL) and so on 3.87 F (%) / 61.5 VSS (L/kg) = 1.13 6.37 / CL (L/h / kg) 5.65 /
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Ba/F3-TEL-FGFR4 cells Tested Concentrations: 0, 50, 100, 200 and 400 nM Incubation Duration: 4 h Experimental Results: demonstrated dose-dependent inhibition of the FGFR4 signal cassette, including the phosphorylation of FGFR4 and its downstream effectors FRS2 and PLCγ. |
Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice, HUH7 xenograft model[1]
Doses: 30 and 45 mg/kg Route of Administration: intragastric (po) gavage; daily for 3 weeks Experimental Results: Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed. Animal/Disease Models: Male CD-1 mice[1] Doses: 1 mg/kg and 10 mg/kg Route of Administration: iv and po (pharmacokinetic/PK Analysis) Experimental Results: demonstrated good in vivo pharmacokinetic/PK profile. |
References |
[1]. Xie W, et al. Discovery of 2-Amino-7-sulfonyl-7 H-pyrrolo [2, 3-d] pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation. Journal of Medicinal Chemistry, 2022.
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Molecular Formula |
C25H28N6O3S
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Molecular Weight |
492.59
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0301 mL | 10.1504 mL | 20.3009 mL | |
5 mM | 0.4060 mL | 2.0301 mL | 4.0602 mL | |
10 mM | 0.2030 mL | 1.0150 mL | 2.0301 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.