O-Desmethyl gefitinib D8

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S0846-2 Contact sales@xcessbio.com for quotation ¥100
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S0846-10 Contact sales@xcessbio.com for quotation ¥100
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详情描述

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.

Product information

Molecular Weight: 440.93

Formula: C21H22ClFN4O3

Chemical Name: 4-[(3-chloro-4-fluorophenyl)amino]-6-{3-[(2, 2, 3, 3, 5, 5, 6, 6-H)morpholin-4-yl]propoxy}quinazolin-7-ol

Smiles: [2H]C1([2H])N(CCCOC2=CC3=C(NC4=CC(Cl)=C(F)C=C4)N=CN=C3C=C2O)C([2H])([2H])C([2H])([2H])OC1([2H])[2H]

InChiKey: IFMMYZUUCFPEHR-RHDPTBQRSA-N

InChi: InChI=1S/C21H22ClFN4O3/c22-16-10-14(2-3-17(16)23)26-21-15-11-20(19(28)12-18(15)24-13-25-21)30-7-1-4-27-5-8-29-9-6-27/h2-3,10-13,28H,1,4-9H2,(H,24,25,26)/i5D2,6D2,8D2,9D2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

  1. Kobayashi H, et al. Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinib. Med Oncol. 2016 Jun;33(6):57.
  2. McKillop D, et al. Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica. 2006 Jan;36(1):29-39.

Products are for research use only. Not for human use.

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