2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. O-Desmethyl gefitinib-d8

O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

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O-Desmethyl gefitinib-d<sub>8</sub> Chemical Structure

O-Desmethyl gefitinib-d8 Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

IC50 & Target

IC50: 36 nM (EGFR)[2]
Molecular Weight

440.93

Formula

C21H14D8ClFN4O3
Unlabeled CAS

847949-49-9
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4C([2H])([2H])C([2H])([2H])OC([2H])([2H])C4([2H])[2H]
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Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (226.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2679 mL 11.3397 mL 22.6793 mL
5 mM 0.4536 mL 2.2679 mL 4.5359 mL
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.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2679 mL 11.3397 mL 22.6793 mL 56.6983 mL
5 mM 0.4536 mL 2.2679 mL 4.5359 mL 11.3397 mL
10 mM 0.2268 mL 1.1340 mL 2.2679 mL 5.6698 mL
15 mM 0.1512 mL 0.7560 mL 1.5120 mL 3.7799 mL
20 mM 0.1134 mL 0.5670 mL 1.1340 mL 2.8349 mL
25 mM 0.0907 mL 0.4536 mL 0.9072 mL 2.2679 mL
30 mM 0.0756 mL 0.3780 mL 0.7560 mL 1.8899 mL
40 mM 0.0567 mL 0.2835 mL 0.5670 mL 1.4175 mL
50 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1340 mL
60 mM 0.0378 mL 0.1890 mL 0.3780 mL 0.9450 mL
80 mM 0.0283 mL 0.1417 mL 0.2835 mL 0.7087 mL
100 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.5670 mL
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O-Desmethyl gefitinib-d8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

O-Desmethyl gefitinib-d8EGFREpidermal growth factor receptorErbB-1HER1DeuteriumlabeledmetaboliteCYP2D6Inhibitorinhibitorinhibit

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