| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EGFR tyrosine kinase[1]
Befotertinib targets the epidermal growth factor receptor (EGFR), specifically the mutant form T790M. It is a potent, selective, and irreversible third-generation EGFR-TKI designed to overcome T790M-mediated resistance. By specifically binding to and inhibiting EGFR T790M, it prevents EGFR-mediated signaling and leads to cell death in tumor cells expressing this resistance mutation. |
|---|---|
| ln Vitro |
In vitro, Befotertinib has been shown to exert antiproliferative effects. It inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. These activities contribute to its potential as a therapeutic agent.
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| ln Vivo |
In vivo, Befotertinib has demonstrated antitumor activity in preclinical models. Its oral bioavailability and potent activity against the T790M mutation support its evaluation in clinical settings for the treatment of EGFR T790M-positive non-small cell lung cancer. It may have therapeutic benefits in tumors with T790M-mediated drug resistance.
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| Enzyme Assay |
Cell-free assays for Befotertinib typically involve measuring its inhibitory activity against wild-type and mutant EGFR kinases using biochemical kinase assays. The compound's IC50 values are determined by measuring the phosphorylation of a substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and selectivity.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Befotertinib. NSCLC cell lines harboring the T790M mutation are treated with the compound. Cell viability and proliferation are measured to assess the compound's anti-proliferative effects. EGFR phosphorylation is also measured to confirm inhibition of the target kinase.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of NSCLC with the T790M mutation. Mice bearing these tumors are administered Befotertinib orally. Tumor growth is monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo antitumor activity of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Befotertinib are characteristic of an orally bioavailable small molecule inhibitor. Its CAS number is 1835667-63-4. The compound is designed to have favorable drug-like properties, including good oral bioavailability and metabolic stability, to support once-daily dosing.
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| Toxicity/Toxicokinetics |
The toxicity profile of Befotertinib is likely consistent with other third-generation EGFR TKIs. Common adverse effects may include diarrhea, skin rash, and fatigue. Its selectivity for the T790M mutation over wild-type EGFR may lead to a more favorable safety profile with reduced skin and gastrointestinal toxicities.
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| References | |
| Additional Infomation |
Befotertinib is an oral inhibitor of the epidermal growth factor receptor (EGFR) T790M mutant with potential antitumor activity. After administration, Befotertinib specifically binds to and inhibits EGFR T790M (a secondary resistance mutation), thereby blocking EGFR-mediated signaling and leading to the death of tumor cells expressing EGFR T790M. Compared to some other EGFR inhibitors, Befotertinib may offer a therapeutic advantage against T790M-mediated resistant tumors. EGFR is a receptor tyrosine kinase that is mutated in various tumor cell types and plays a crucial role in tumor cell proliferation and tumor angiogenesis.
Befotertinib is a third-generation EGFR TKI developed to overcome T790M-mediated resistance in NSCLC. Its mechanism of action involves irreversible binding to mutant EGFR. The compound is currently in clinical development for the treatment of EGFR-mutant NSCLC. It represents a promising therapeutic option for patients who have developed resistance to earlier-generation EGFR inhibitors. |
| Molecular Formula |
C29H32F3N7O2
|
|---|---|
| Molecular Weight |
567.605296134949
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| Exact Mass |
567.256
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| CAS # |
1835667-63-4
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| PubChem CID |
130412842
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
863
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(CN1C=C(C2C=CN=C(N=2)NC2=CC(=C(C=C2OC)N(C)CCN(C)C)NC(C=C)=O)C2C=CC=CC1=2)(F)F
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| InChi Key |
USOCZVZOXKTJTI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H32F3N7O2/c1-6-27(40)34-22-15-23(26(41-5)16-25(22)38(4)14-13-37(2)3)36-28-33-12-11-21(35-28)20-17-39(18-29(30,31)32)24-10-8-7-9-19(20)24/h6-12,15-17H,1,13-14,18H2,2-5H3,(H,34,40)(H,33,35,36)
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| Chemical Name |
N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-[1-(2,2,2-trifluoroethyl)indol-3-yl]pyrimidin-2-yl]amino]phenyl]prop-2-enamide
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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: 50 mg/mL (88.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.66 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 | 1.7618 mL | 8.8089 mL | 17.6177 mL | |
| 5 mM | 0.3524 mL | 1.7618 mL | 3.5235 mL | |
| 10 mM | 0.1762 mL | 0.8809 mL | 1.7618 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.
Link: https://clinicaltrials.gov/ct2/show/NCT07410611
Conditions:Patients With Advanced Oligometastatic Non-small Cell Lung Cancer (NSCLC) Who Have Tested Positive for EGFR Mutations Confirmed by Histopathological ExaminationLink: https://clinicaltrials.gov/ct2/show/NCT07181499
Conditions:NSCLC|Adjuvant Drug Therapy|EGFRLink: https://clinicaltrials.gov/ct2/show/NCT04206072
Conditions:Non-Small Cell Lung Cancer|EGFR Gene Mutation
Title:Phase II Clinical Study of Befotertinib in EGFR Non-classical Mutant NSCLC
Status:Recruiting
updateDate:2025-03-07
Ctid:NCT06863506
Link: https://clinicaltrials.gov/ct2/show/NCT06863506
Conditions:NSCLC (Non-small Cell Lung Cancer)Link: https://clinicaltrials.gov/ct2/show/NCT05007938
Conditions:Non-Small Cell Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT06561620
Conditions:3-year Disease-free SurvivalLink: https://clinicaltrials.gov/ct2/show/NCT06517953
Conditions:Non-small Cell Lung Cancer Metastatic|EGFR G719X|EGFR L861Q|EGFR S768ILink: https://clinicaltrials.gov/ct2/show/NCT03861156
Conditions:Solid Tumor|NSCLC|EGFR T790MLink: https://clinicaltrials.gov/ct2/show/NCT06041776
Conditions:Non-Small Cell Lung Cancer|EGFR Sensitive Mutation|Adjuvant TherapyLink: https://clinicaltrials.gov/ct2/show/NCT03452150
Conditions:Advanced Non Small Cell Lung CancerProducts are for research use only; We do not sell to patients
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