| Company Name: |
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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| Tel: |
17702719238 17702719238 |
| Email: |
sales@sun-shinechem.com |
| Products Intro: |
Product Name:limertinib (ASK120067)
CAS:1934259-00-3
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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| Company Name: |
Chunchuang (Wuhan) Technology Co., Ltd
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| Tel: |
15342225168 |
| Email: |
yutianchun2007@126.com |
| Products Intro: |
Product Name:2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]-
CAS:1934259-00-3
Purity:99.5+ Package:1g/RMB 100
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:ASK120067;ASK120067,ASK-120067
CAS:1934259-00-3
Purity:98% Package:100 mg;25 mg;50 mg
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| Company Name: |
Accela ChemBio Co.,Ltd.
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| Tel: |
021-50795510 4000665055 |
| Email: |
SY06@accelachem.com |
| Products Intro: |
Product Name:N-[5-[[5-Chloro-4-(2-naphthylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl](methyl)amino]-4-methoxyphenyl]acrylamide
CAS:1934259-00-3
Purity:>=95% Package:1g
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| | 2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- Basic information |
| | 2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- Chemical Properties |
| density | 1.307±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (183.13 mM; Need ultrasonic) | | pka | 12.65±0.70(Predicted) | | form | Solid | | color | White to yellow |
| | 2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- Usage And Synthesis |
| 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]. | | 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. |
| | 2-Propenamide, N-[5-[[5-chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]- Preparation Products And Raw materials |
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