Afatinib Dimaleate

SKU: orb1307469

Description

Afatinib Dimaleate is an orally active, irreversible inhibitor of the ErbB (EGFR) family of receptor tyrosine kinases. This small molecule is used in research to study oncogenic signaling and has demonstrated antitumor activity in both cellular assays and animal models of non-small cell lung cancer and other solid tumors.

Research Area

Pharmacology & Drug Discovery

Images & Validation

−

Key Properties

−

CAS Number	850140-73-7
MW	718.08
Purity	>99.99% (May vary between batches)
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	Apoptosis,Autophagy,Akt,HER,c-Met/HGFR,p38 MAPK,EGFR
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. Read more...
In Vitro	In the MDA-MB-453 transplantation tumor model, oral administration of Afatinib (20 mg/kg), which down-regulated 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. Read more...
Cell Research	Cytotoxicity is determined using MTT assay. The IC 50 value is de ned as the drug concentration resulting in 50% cell death. Both the tted sigmoidal dose response curve and IC50 are calculated by Bliss method.(Only for Reference) Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
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

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

15606394 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols