S-22611 free base · Synonyms: Epertinib | S-22611

Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM…

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

S-22611 structure

CAS No.: 908305-13-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 530.00	BP-02515-5mg	In stock	Get quote
10 mg	USD 950.00	BP-02515-10mg	In stock	Get quote
50 mg	USD 1,900.00	BP-02515-50mg	In stock	Get quote
100 mg	USD 2,900.00	BP-02515-100mg	In stock	Get quote
250 mg	Inquire	BP-02515-250mg	In stock	Inquire

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Description

Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity . Epertinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Biological activity

In Vitro Epertinib inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively. Epertinib shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM. Epertinib (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2. In Vivo Epertinib (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity. Epertinib (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume. Epertinib (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner.

Identifiers

SMILES: CC#CC(=N/OC[C@H]1COCCN1)\C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1
InChIKey: IBCIAMOTBDGBJN-NRLRZRKLSA-N

Specifications

MW (average): 560.0180
Formula: C₃₀H₂₇ClFN₅O₃
CAS No.: 908305-13-5
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, protect from light

Solubility

Soluble in DMSO

Documents

References

[1].Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343.

[2].Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8.

Same target

Search EGFR

Same research area

Search Cancer