Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
EGFRL858R/T790M
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ln Vitro |
Compound 24, also known as EGFR-IN-1 TFA, is an irreversible and oral EGFR inhibitor that selectively targets the L858R/T790M mutation. Gefitinib-resistant EGFR L858R, T790M are potently inhibited by EGFR-IN-1 TFA, which exhibits 100-fold selectivity over wild-type EGFR. Strong antiproliferative activity of EGFR-IN-1 TFA is observed against H1975 cells and the first line mutant HCC827 cells. activity against tumors[1].
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ln Vivo |
EGFR-IN-1 TFA (30 mg/kg; po; daily for 2 weeks) significantly inhibits the growth of tumors while not causing weight loss[1]. After oral dosage at 30 mg/kg, EGFR-IN-1 TFA is evaluated in a time-course PD experiment. For more than 12 hours, EGFR-IN-1 TFA exhibits a >50% suppression of EGFR phosphorylation. At two hours, the maximum concentration of EGFR-IN-1 TFA is 0.10 μM, while the systemic exposure (AUC0-inf.) is 0.33 μM. Hi[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: NSCLC cell lines H1975 (T790M/L858R), HCC827 (Δ 746-750) Tested Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively. |
References |
[1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.
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Molecular Formula |
C30H31F3N6O6
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Molecular Weight |
628.60
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CAS # |
2753348-63-7
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Related CAS # |
EGFR-IN-1;1625677-63-5;EGFR-IN-1 hydrochloride;2227455-78-7
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: 250 mg/mL (397.71 mM)
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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 | 1.5908 mL | 7.9542 mL | 15.9084 mL | |
5 mM | 0.3182 mL | 1.5908 mL | 3.1817 mL | |
10 mM | 0.1591 mL | 0.7954 mL | 1.5908 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.