Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 6-8 weeks | $ 197.00 | |
25 mg | 6-8 weeks | $ 670.00 | |
50 mg | 6-8 weeks | $ 871.00 | |
100 mg | 6-8 weeks | $ 1,240.00 |
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]. |
Targets&IC50 | EGFR (WT):6 nM (IC50), EGFR (T790M):0.5 nM (IC50), EGFR (exon 19 deletion):0.5 nM (IC50), EGFR (L858R/T790M):0.3 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]. |
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]. |
Molecular Weight | 546.06 |
Formula | C29H32ClN7O2 |
CAS No. | 1934259-00-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (183.13 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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ASK120067 1934259-00-3 ASK 120067 ASK-120067 inhibitor inhibit