EGF816 is Solid powder, while it's Molecular Formula is C26H31ClN6O2. Solid powder

What is the CAS number for EGF816?

The CAS number of EGF816 is 1508250-71-2.

What is EGF816 (1508250-71-2) used for?

Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC50 = 4.18 nM), over cells expressing wild-type EGFRs (IC50 = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC50s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.

EGF816 is Solid powder, while it's Molecular Formula is C26H31ClN6O2. Solid powder

What is the CAS number for EGF816?

The CAS number of EGF816 is 1508250-71-2.

What is EGF816 (1508250-71-2) used for?

Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC50 = 4.18 nM), over cells expressing wild-type EGFRs (IC50 = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC50s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.

1508250-71-2

Product Name：EGF816
Molecular Formula：C26H31ClN6O2
Purity：99%
Molecular Weight：495.02

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Product Details

CasNo： 1508250-71-2

Molecular Formula： C26H31ClN6O2

Appearance： Solid powder

Quality Manufacturer Supply EGF816, Buy 1508250-71-2 Safe Transportation

Molecular Formula:C26H31ClN6O2
Molecular Weight:495.02
Appearance/Colour:Solid powder
PKA:11.38±0.43(Predicted)
PSA：83.36000
Density:1.28±0.1 g/cm3(Predicted)
LogP:4.32770

EGF816 (Cas 1508250-71-2) Usage

EGF816, also known as nazartinib, is a covalent, irreversible, third-generation EGFR TKI (epidermal growth factor receptor tyrosine kinase inhibitor). It has activity against EGFR activating and Thr790Met mutations, while sparing wild-type EGFR. It exerts anticancer effects in non-small cell lung cancer.

1508250-71-2 Relevant articles

Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816

Gerald Lelais; Robert Epple; Pierre-Yves Michellys; Thomas H. Marsilje; Yun Long; Matthew McNeill; Bei Chen; Wenshuo Lu; Badry Bursulaya; Michael DiDonato; Yong Jia; Shailaja Kasibhatla; Chun Li; Igor Matushansky; Steven Bender

, Cancer Res (2015) 75 (15_Supplement): 2585.

In this presentation, we report our medicinal chemistry approach and optimization that led to the discovery of EGF816, a selective and potent covalent mutant-selective EGFR inhibitor with single digit nanomolar cellular target modulation on both activating and T790M resistance mutations.

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