1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. ASK120067

ASK120067 

Cat. No.: HY-138751
Handling Instructions

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).

For research use only. We do not sell to patients.

ASK120067 Chemical Structure

ASK120067 Chemical Structure

CAS No. : 1934259-00-3

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Description

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRT790M

0.5 nM (IC50)

EGFRL858R/T790M

0.3 nM (IC50)

EGFR (WT)

6 nM (IC50)

EGFRExon 19 deletion

0.5 nM (IC50)

In Vitro

In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT) is 6 nM[1].
ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].
ASK120067 (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ASK120067 (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/cA nude mice[1]
Dosage: 5-20 mg/kg
Administration: Oral gavage; 5-20 mg/kg; once daily; 21 days
Result: Were well tolerated in animals without observed body weight loss
Demonstrated profound and selective antitumor efficacy and decreased TGI rate.
Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.
Molecular Weight

546.06

Formula

C₂₉H₃₂ClN₇O₂

CAS No.
SMILES

O=C(NC1=CC(NC2=NC=C(C(NC3=CC4=C(C=CC=C4)C=C3)=N2)Cl)=C(C=C1N(CCN(C)C)C)OC)C=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ASK120067ASK 120067ASK-120067EGFREpidermal growth factor receptorErbB-1HER1NSCLClung cancerEGFR T790MMetastatic NSCLCEGFR-TKIInhibitorinhibitorinhibit

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ASK120067
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