| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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| ln Vitro |
The anti-proliferative efficacy of PROTAC is demonstrated by PROTAC EGFR degrader 3 (compound CP17), which has an IC50 of 32 nM, 1.60 nM, and >10000 nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), and A431 (EGFRWT) cells, respectively [1]. Poor cellular activity was seen with PROTAC EGFR Degrader 3 (0, 10, 100, 1000, and 10,000 nM), with an IC50 of 481 for Ba/F3 (EGFRdel19/T790M/C797S) and Ba/F3 (EGFRL858/T790M/C797S). nM and 669 nM cells, in that order [1]. The growth of PC9 (EGFRdel19/T790M/C797S) and H1975 (EGFRL858/T790M/C797S) cells is inhibited by PROTAC EGFR degrader 3 (0-10000 nM), respectively [1]. EGFRL858/T790M expression is reduced by PROTAC EGFR Degrader 3 (30 nM; 0-72 hours) after 8 hours, and the degradation rate reaches its peak after 48 hours [1]. EGFRL858/T790M and EGFRdel19 are degraded by PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h), with a DC50 of 1.56 nM and 0.49 nM, respectively [1]. In H1975 and HCC827 cells, PROTAC EGFR Degrader 3 (100, 1000 nM; 24 hours) exhibits selectivity against mutant EGFR [1]. Cell growth is inhibited by PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, and 300 nM; 24 hours), which efficiently suppresses EGFR signal transduction [1]. EGFR mutations are degraded by PROTAC EGFR degrader 3 (30 nM), and lysosomes take part in this process [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) Cell Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: PROTAC demonstrated anti-proliferative activity with IC50 of 32 nM, 1.60 nM for H1975 (EGFRL858/T790M), HCC827 (EGFRdel19), A431 (EGFRWT) cells, >10000nM respectively. Western Blot Analysis [1] Cell Types: H1975, HCC827 Cell Tested Concentrations: 0.3, 1, 3, 10, 30 nM Incubation Duration: 24 h Experimental Results: Phosphorylated EGFR, ERK, and AKT were Dramatically diminished in H1975 and HCC827 cells. |
| References |
| Molecular Formula |
C60H77N13O5S
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|---|---|
| Molecular Weight |
1092.40
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| CAS # |
2768472-28-0
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| Appearance |
Off-white to light yellow solid powder
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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 : ~100 mg/mL (~91.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.29 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 25.0 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 | 0.9154 mL | 4.5771 mL | 9.1542 mL | |
| 5 mM | 0.1831 mL | 0.9154 mL | 1.8308 mL | |
| 10 mM | 0.0915 mL | 0.4577 mL | 0.9154 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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