| ln Vitro |
FGFR-IN-26 (compound 13) (dose-response series) effectively inhibits the proliferation of Ba/F3 cells expressing FGFR1, FGFR2 (wild-type and clinically relevant drug-resistant mutations), FGFR3 and FGFR4. It has the highest efficacy against FGFR2K660E (IC50 = 0.6 nM) and FGFR3 (IC50 = 0.2 nM), and its selectivity for FGFR2 is 23 times higher than that for FGFR4 [1]. FGFR-IN-26 can effectively bind to FGFR2 (Kd = 2.7 nM), FGFR2(N550K) (Kd = 10 nM), FGFR1 (Kd = 21 nM) and FGFR3 (Kd = 3.5 nM), with a selectivity for FGFR2 that is 85 times higher than that for FGFR4, and a weaker and reversible binding to FGFR2(C491F) (Kd = 956 nM), which is consistent with the covalent mechanism [1]. FGFR-IN-26 (72-120 h) can effectively inhibit the activity of FGFR2-driven SNU-16 gastric cancer cells (IC50 = 7.5 nM) and AN3CA endometrial cancer cells carrying the FGFR2N550K mutation (IC50 = 13 nM) [1]. FGFR-IN-26 (1 μM) exhibits high selectivity for the human kinase community, inhibiting more than 90% of only 13 wild-type kinases [1].
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| ln Vivo |
FGFR-IN-26 (compound 13) (10 mg/kg; orally; twice daily; 21 days) achieved 152% tumor growth inhibition in a nude mouse model of FGFR2-amplified SNU-16 gastric cancer xenograft without significant weight loss [1].
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| Animal Protocol |
Animal/Disease Models:Nude mice (female, 6-8 weeks old) with FGFR2 amplified SNU-16 gastric cancer xenograft model [1]
Doses: 10 mg/kg< Route of Administration:Oral; twice daily; for 21 days Experimental Results:Tumor growth inhibition rate (TGI) reached 152% within 21 days. Four hours after the last administration, the plasma drug concentration reached 192 ng/mL (480 nM). No significant weight loss was observed after 21 days. |
| References |
| CAS # |
2823290-68-0
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|---|---|
| Appearance |
Typically exists as solids 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.) |
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.
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