Dacomitinib [1110813-31-4]
Cat# HY-13272-10mg
Size : 10mg
Brand : MedChemExpress
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
For research use only. We do not sell to patients.
Dacomitinib Chemical Structure
CAS No. : 1110813-31-4
This product is a controlled substance and not for sale in your territory.
Based on 17 publication(s) in Google Scholar
Other Forms of Dacomitinib:
- Dacomitinib hydrate In-stock
- Dacomitinib-d10 dihydrochloride Get quote
- Dacomitinib-d10 Get quote
Description |
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1]. |
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IC50 & Target |
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In Vitro |
Dacomitinib (PF00299804) effectively inhibits the in vitro kinase activity of wild-type EGFR (IC50=6 nM)with similar efficacy. Dacomitinib also effectively inhibits wild-type ERBB2 with IC50 of 45.7 nM. In H441, an IC50 is reached with Dacomitinib but only at a very high concentration (4 μM) and likely reflects off-target effects. In cell lines wild-type for both EGFR and K-ras (H322, H1819, and Calu-3), ZD1839 and Dacomitinib both effectively inhibit growth of H1819 and Calu-3 cells but not of H322 cells. Dacomitinib is a pan-ERBB inhibitor and most EGFR mutant cell lines express multiple ERBB family members, the effects on EGFR phosphorylation could potentially be indirect. Dacomitinib inhibits EGFR phosphorylation in all of the different EGFR T790M proteins whereas ZD1839 is ineffective even at 10 μM. In the NIH3T3 cells, phosphorylation of EGFR L858R/T790M is completely inhibited by 1 nM Dacomitinib, whereas 100 nM or greater is required to inhibit EGFR WT/T790M or Del/T790M[1]. The HER2-amplified cell lines are most sensitive to growth inhibition by Dacomitinib (IC50<1 μM in 14 of 16 lines; 87.5%) as compared with 5 of 28 (17.9%) of HER2-nonamplified lines (excluding immortalized lines)[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
To evaluate the efficacy of Dacomitinib, xenografts in nu/nu mice are generated using HCC827 GFP and HCC827 Del/T790M cells and treated the mice with Dacomitinib. Dacomitinib (10 mg/kg/d by daily oral gavage) effectively inhibits the growth of HCC827 GFP xenografts. In contrast, HCC827 Del/T790M xenografts are resistant to ZD1839, whereas Dacomitinib treatment is substantially more effective at inhibiting growth of this xenograft model[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
469.94 |
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Formula |
C24H25ClFN5O2 |
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CAS No. |
1110813-31-4 |
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Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 40 mg/mL (85.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Purity & Documentation | |||||||||||||
References |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1279 mL | 10.6397 mL | 21.2793 mL | 53.1983 mL |
5 mM | 0.4256 mL | 2.1279 mL | 4.2559 mL | 10.6397 mL | |
10 mM | 0.2128 mL | 1.0640 mL | 2.1279 mL | 5.3198 mL | |
15 mM | 0.1419 mL | 0.7093 mL | 1.4186 mL | 3.5466 mL | |
20 mM | 0.1064 mL | 0.5320 mL | 1.0640 mL | 2.6599 mL | |
25 mM | 0.0851 mL | 0.4256 mL | 0.8512 mL | 2.1279 mL | |
30 mM | 0.0709 mL | 0.3547 mL | 0.7093 mL | 1.7733 mL | |
40 mM | 0.0532 mL | 0.2660 mL | 0.5320 mL | 1.3300 mL | |
50 mM | 0.0426 mL | 0.2128 mL | 0.4256 mL | 1.0640 mL | |
60 mM | 0.0355 mL | 0.1773 mL | 0.3547 mL | 0.8866 mL | |
80 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6650 mL |