| ln Vitro |
FGFR3-IN-11 (B10) (48 hours) effectively inhibited the proliferation of Huh-7, HepG2 and MHCC97-H liver cancer cell lines, with IC50 values of 4.13, 4.76 and 5.79 μM, respectively, and showed very low toxicity to L02 normal hepatocytes [1]. FGFR3-IN-11 (B10) (1.25-5 μM; initial treatment for 48 hours, followed by culture medium replacement every 14 days) inhibited the colony formation of Huh-7 liver cancer cells in a dose-dependent manner [1]. FGFR3-IN-11 (B10) (1.25-5 μM; 48 hours) induced G0/G1 phase arrest in Huh-7 liver cancer cells in a dose-dependent manner [1]. FGFR3-IN-11 (B10) (1.25-5 μM; 24 hours) can induce apoptosis in Huh-7 hepatocellular carcinoma cells in a dose-dependent manner, accompanied by corresponding changes in the levels of Bcl-2 and Bax proteins [1]. FGFR3-IN-11 (B10) (1.25-5 μM; 24 hours) can inhibit the PI3K/AKT signaling pathway by dose-dependently reducing the levels of total PI3K and AKT, as well as phosphorylated PI3K and AKT in Huh-7 hepatocellular carcinoma cells [1]. FGFR3-IN-11 (B10) (serial dilutions, 40 μM, 10-40 μM; pre-incubated with DARTS for 1 hour) can stably bind to FGFR3 protein with a dissociation constant (KD) of 4.8 μM, which was verified by molecular docking, SPR, CETSA and DARTS experiments [1].
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| ln Vivo |
B10 (20-60 mg/kg; intraperitoneal injection; every other day; 28 days) showed strong in vivo antitumor efficacy in the Huh-7 xenograft model, with a TGI rate of 64.18% at 40 mg/kg and good safety [1].
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| Animal Protocol |
Animal/Disease Models:Balb/c nude mice (female, 4-6 weeks old, average weight 18-19 g) [1]
Doses: 20, 40, 60 mg/kg; 40 mg/kg (tumor growth inhibition rate assessment) Route of Administration: Intraperitoneal injection; every other day; 28 days Experimental Results: The tumor growth inhibition rate (TGI) reached 64.18% at a dose of 40 mg/kg; induced a dose-dependent decrease in phosphorylated FGFR3 (p-FGFR3) in tumor tissue; resulted in a significant reduction in Ki-67 positive cells in the tumor; no significant weight loss was observed compared with the control group. |
| References |
| 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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