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Oritinib
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Catalog No. T60076Cas No. 2035089-28-0
Alias SH-1028
Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.
Oritinib
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Purity: 99.62%
Catalog No. T60076Alias SH-1028Cas No. 2035089-28-0
Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $136 | In Stock | In Stock | |
| 5 mg | $338 | In Stock | In Stock | |
| 10 mg | $493 | In Stock | In Stock | |
| 25 mg | $818 | In Stock | In Stock | |
| 50 mg | $1,090 | In Stock | In Stock | |
| 100 mg | $1,490 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $393 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.62%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer. |
| Targets&IC50 | EGFR (L861Q):4 nM, EGFR (d746-750/T790M):0.89 nM, EGFR (d746-750):1.4 nM, EGFR (WT):18 nM, EGFR L858R:0.7 nM, EGFR L858R/T790M:0.1 nM |
| In vitro | Oritinib (0.001, 0.01, 0.1, 1, and 10 μM) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50s of 3.932, 9.39 and 7.63 nM, respectively. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells[1]. |
| In vivo | In female mice bearing NCI-H1975 and A431 xenograft models， Oritinib (2.5, 5, and 15 mg/kg; oral) significantly inhibits proliferation of tumor cells with no TKI-induced weight loss. In NCI-H1975 tumor-bearing mice, Oritinib (2.5, 5, and 15 mg/kg; oral) shows good bioavailability(Tmax = 1.5-2 h) and extensive distribution from the plasma to the tissues. The AUC0–t values in plasma are 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively[1]. |
| Synonyms | SH-1028 |
| Molecular Weight | 539.67 |
| Formula | C31H37N7O2 |
| Cas No. | 2035089-28-0 |
| Smiles | COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1c2CCCCn2c2ccccc12 |
| Relative Density. | 1.22 g/cm3 (Predicted) |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (222.36 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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