| Company Name: |
hubei PharmaStandard Co., Ltd. Gold
|
| Tel: |
027-19050701 13545374703 |
| Email: |
cbbspring@163.com |
| Products Intro: |
Product Name:JBJ-09-063
CAS:2820336-67-0
Purity:97% HPLC Package:50mg,100mg, 500mg
|
| Company Name: |
Chunchuang (Wuhan) Technology Co., Ltd
|
| Tel: |
15727060112 |
| Email: |
yutianchun2007@126.com |
| Products Intro: |
Product Name:2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl-
CAS:2820336-67-0
|
|
| | 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Basic information |
| | 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Chemical Properties |
| density | 1.372±0.06 g/cm3(Predicted) | | pka | 7.21±0.50(Predicted) | | InChIKey | SYTVDTWRIZNVEW-UHFFFAOYSA-N | | SMILES | C(C1C=C(F)C=CC=1O)(N1CC2=CC=C(C3C=CC(C4CCN(C)CC4)=CC=3)C=C2C1=O)C(=O)NC1SC=CN=1 |
| | 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Usage And Synthesis |
| Uses | JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer[1]. | | in vivo | JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing[2]. | Animal Model: | Mice[2] | | Dosage: | 3 mg/kg for i.v., 20 mg/kg for p.o. | | Administration: | i.v. and p.o.; single dosage | | Result: | Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
| Cl (mL/min/kg), i.v. | T1/2 (h) | Vss (L/kg) | F (%) | AUC 8h (ng·h/mL) | | 15.7 | 2.3 | 2.5 | 15 | 2398 |
|
| | IC 50 | EGFR L858R: 0.147 nM (IC50); EGFR L858R/T790M: 0.063 nM (IC50); EGFR L858R/T790M/C797S: 0.083 nM (IC50); EGFRLT/L747S: 0.396 nM (IC50) | | References | [1] To C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417. DOI:10.1038/s43018-022-00351-8 |
| | 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Preparation Products And Raw materials |
|