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EGFR-IN-1 hydrochloride

Catalog No. T11157L CAS 2227455-78-7

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity in H1975 cells and the mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.

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EGFR-IN-1 hydrochloride Chemical Structure

EGFR-IN-1 hydrochloride, CAS 2227455-78-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 173.00
5 mg	In stock	$ 427.00
10 mg	In stock	$ 632.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,350.00
100 mg	In stock	$ 1,830.00
500 mg	In stock	$ 3,660.00
1 mL * 10 mM (in DMSO)	In stock	$ 591.00

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Purity: 99.8%

Biological Description

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Storage & Solubility Information

Description	EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity in H1975 cells and the mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.
Targets&IC50	p-EGFR:4-9nM
In vitro	EGFR-IN-1 is highly selective against a panel of 100 kinases and inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively[1].
In vivo	In female athymic nude mice with H1975 Tumor Xenograft, gavage administration of EGFR-IN-1 hydrochloride (30 mg/kg) significantly inhibits the tumor growth without observed loss in body weight. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR and a systemic exposure (AUC0-inf.) of 0.33 μM. h[1].

Molecular Weight	551.04
Formula	C28H31ClN6O4
CAS No.	2227455-78-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (18.15 mM)

References and Literature

1. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

EGFR-IN-1 hydrochloride 2227455-78-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR EGFR-IN-1 Hydrochloride EGFRIN1 hydrochloride EGFR IN 1 hydrochloride inhibitor inhibit

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