Afatinib Dimaleate

SKU: orb1307469

Description

Afatinib Dimaleate

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 850140-73-7
• MW: 718.08
• Purity: 99.87%
• Formula: C₃₂H₃₃ClFN₅O₁₁
• SMILES: OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CN(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1
• Target: EGFR,Autophagy,Akt,HER,c-Met/HGFR,Apoptosis,p38 MAPK
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:252 mg/mL (350.94 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR (WT):0.5 nM|EGFR (L858R):0.4 nM|HER2:14 nM|EGFR (L858R/T790M):10 nM
• In Vivo:
  In lung cancer cell lines expressing wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, Afatinib inhibited cell growth more effectively. In NSCLC cell lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), Afatinib was more effective in inhibiting cell growth.
• In Vitro:
  I the MDA-MB-453 transplantation tumor model, oral administration of Afatinib (20 mg/kg), which down-regulate the phosphorylation levels of EGFR and AKT, induced tumor regression. in the NCI-N87 transplantation model of HER2-positive gastric cancer, oral administration of Afatinib (25 mg/kg) was able to eliminate tumors. In A7, A431, FaDu, UT-SCC-14 and UT-SCC-15 transplantation tumor models, oral administration of Afatinib (30 mg/kg) inhibited tumor growth.
• Cell Research:
  Cytotoxicity is determined using MTT assay the IC 50 value is defined a the drug concentration resulting in 50% cell death. Bot the fitted sigmoidal dose response curve and IC50 are calculated by Bliss method.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, NCI-H1975, NIH-3T3 cells, NSCLC, orally active, lung cancer, HER2, HER1, Inhibitor, HKESC-1, HKESC-2, H1666, H3255, EGFR (L858R/T790M), EGFR (L858R), EGFR (wt), EC-1, EGFR, ErbB-1, Epidermal growth factor receptor, ESCC, Autophagy, Apoptosis, anticancer, BIBW 2992, BIBW 2992MA2, BIBW2992, BIBW-2992, A431, Afatinib Dimaleate, Afatinib, Afatinib (BIBW2992), Afatinib (BIBW2992) Dimaleate, Akt, c-Met/HGFR, SLMT-1, Protein kinase B, PKB, p38 MAPK

Compound Identifiers

PubChem CID

15606394