| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
EGFR
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|---|---|
| ln Vitro |
In cell lines with GI50 values of 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M), and > 1000 nM (A431, EGFR WT), rezivertinib (BPI-7711) specifically inhibits the cellular proliferation of EGFR mutations[1].
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| ln Vivo |
Significant tumor regression is observed when rezivertinib (BPI-7711; 6.25–25 mg/kg/day; oral; 14 days) is used[2]. The H1975-luc human NSCLC mouse model had an average survival time of 112% longer when rezivertinib (12.5 mg/kg/day; oral; 14 days) is administered[2]. The anti-tumor activity of rezivertinib (50 mg/kg/day; oral) has been linked to an increase in the animals' average overall survival of 115% (28 days vs. 13 days)[2].
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| References |
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| Additional Infomation |
Rezivertinib is an oral, third-generation selective epidermal growth factor receptor (EGFR) inhibitor that inhibits certain EGFR activating mutations, including resistance mutations T790M and L858R, as well as exon 19 deletions, and possesses potential antitumor activity. After administration, rezivertinib specifically covalently binds to and inhibits specific EGFR mutations, exhibiting particularly high selectivity for the T790M mutation, thereby blocking EGFR mutation-mediated signaling and leading to the death of EGFR-mutant tumor cells. Compared to some other EGFR inhibitors, rezivertinib may offer a therapeutic advantage against T790M-mediated resistant tumors. The drug has very low activity against wild-type EGFR (wt EGFR) and does not cause the dose-limiting toxicities observed with non-selective EGFR inhibitors (which also inhibit wt EGFR). EGFR is a receptor tyrosine kinase that is mutated in many tumor cell types and plays a crucial role in tumor cell proliferation and tumor angiogenesis.
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| Molecular Formula |
C27H30N6O3
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|---|---|
| Molecular Weight |
486.57
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| Exact Mass |
486.237
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| CAS # |
1835667-12-3
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| PubChem CID |
118912975
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.617
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| LogP |
3.53
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
724
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BPMZUKYFIDPLEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30N6O3/c1-6-26(34)29-22-15-21(24(35-5)16-25(22)36-14-13-32(2)3)31-27-28-12-11-20(30-27)19-17-33(4)23-10-8-7-9-18(19)23/h6-12,15-17H,1,13-14H2,2-5H3,(H,29,34)(H,28,30,31)
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| Chemical Name |
N-[2-[2-(dimethylamino)ethoxy]-4-methoxy-5-[[4-(1-methylindol-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: 125 mg/mL (256.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.27 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 (4.27 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 | 2.0552 mL | 10.2760 mL | 20.5520 mL | |
| 5 mM | 0.4110 mL | 2.0552 mL | 4.1104 mL | |
| 10 mM | 0.2055 mL | 1.0276 mL | 2.0552 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.
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