| Identification | Back Directory | [Name]
2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- | [CAS]
1934259-00-3 | [Synonyms]
2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- | [Molecular Formula]
C29H32ClN7O2 | [MDL Number]
MFCD34473275 | [MOL File]
1934259-00-3.mol | [Molecular Weight]
546.07 |
| Chemical Properties | Back Directory | [density ]
1.307±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (183.13 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.65±0.70(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
limertinib (ASK120067) is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of?non-small cell lung cancer (NSCLC)[1]. | [Biological Activity]
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].
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].
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]. | [in vivo]
limertinib (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 limertinib causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[1]. | 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 lossDemonstrated profound and selective antitumor efficacy and decreased TGI rate.Significantly inhibited the phosphorylation of EGFR?L858R/T790M?and AKT in tumor tissue. |
| [IC 50]
EGFRT790M: 0.5 nM (IC50); EGFRL858R/T790M: 0.3 nM (IC50); EGFR (WT): 6 nM (IC50); EGFRExon 19 deletion: 0.5 nM (IC50) | [storage]
Store at -20°C | [References]
[1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90. |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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