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1557268-88-8 (Avitinib (maleate))

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Identification

Avitinib (maleate) Avitinib (maleate)
Name Avitinib (maleate)
Formula C30H30FN7O6
MW 603.6
CAS No. 1557268-88-8
EINECS
Smiles O=C(O)/C=CC(O)=O.O=C(C=C)NC1=CC=CC(OC2=NC(NC3=CC(F)=C(N4CCN(C)CC4)C=C3)=NC5=C2C=CN5)=C1
Synonyms
InChI InChI=1S/C26H26FN7O2.C4H4O4/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34;5-3(6)1-2-4(7)8/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32);1-2H,(H,5,6)(H,7,8)/b;2-1-
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Introduction

Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM.

Background Information

Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (<b>EGFR</b>) inhibitor with an <b>IC<sub>50</sub></b> of 7.68 nM. IC50 & Target: IC50: 7.68 nM (wild-type EGFR)<sup>[1]</sup> <i><b>In Vitro:</b></i> Avitinib is structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors such as osimertinib and rociletinib. Avitinib is designed specifically to inhibit EGFR active mutations and the T790M acquired resistant mutation, while sparing wild type EGFR. Avitinib selectively inhibits EGFR active and T790M mutations with up to 298-fold increase in potency compared to wild-type EGFR. Avitinib exhibits potent inhibitory activity with IC<sub>50</sub> value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC<sub>50</sub>=7.68 nM). Avitinib selectively inhibits mutant EGFR phosphorylation with IC<sub>50</sub> values of 7.3 nM and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431<sup>[1]</sup>. <i><b>In Vivo:</b></i> Oral administration of avitinib at daily dose of 500 mg/kg results in complete remission of tumors with EGFR active and T790M mutations for over 143 days with no weight loss. Three major metabolites of avitinib are tested and show no wild-type EGFR inhibition and off-target effects such as inhibition of IGF-1R. Avitinib is safe in non-small cell lung cancer (NSCLC) patients at the dose range between 50 mg and 550 mg once per day and no hyperglycemia and other severe adverse effects are detected such as grade 3 QT prolongation<sup>[1]</sup>. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000135350

Storage condition

Solubility

DMSO: ≥300 mg/mL by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
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Safety Data of Avitinib (maleate)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
MedChemexpress Co., Ltd. USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
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Related Products

Other Forms of 1557268-88-8

Name CAS No Formula MW

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD 168393 194423-15-9 C17H13BrN4O 369.22
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanic acid 481-74-3 C15H10O4 254.24
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

Protocol Reference

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More Information

Avitinib (maleate)

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