2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl-
![2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Structure](CAS/20211123/GIF/2820336-67-0.gif)
- CAS No.
- 2820336-67-0
- Chemical 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-
- Synonyms
- 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl-
- CBNumber:
- CB912247548
- Molecular Formula:
- C31H29FN4O3S
- Molecular Weight:
- 556.66
- MDL Number:
- MOL File:
- 2820336-67-0.mol
2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- 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- Chemical Properties,Uses,Production
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].
|
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
Raw materials
Preparation Products
2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-6-[4-(1-methyl-4-piperidinyl)phenyl]-1-oxo-N-2-thiazolyl- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| hubei PharmaStandard Co., Ltd. | 027-19050701 13545374703 | cbbspring@163.com | China | 430 | 58 |
| Shanghai Beckham Medical Technology Co., Ltd | 021-13816613772 13816613772 | huahero21@sina.com | China | 2037 | 55 |
| Shanghai Rechem science Co., Ltd. | 021-31433387 15618786686 | sales@rechemscience.com | China | 2957 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15727060112 | yutianchun2007@126.com | China | 9800 | 58 |
| Chengdu PEIP Pharmaceutical Technology Co., LTD. | 028-61715638 18011352545 | 1242335275@qq.com | China | 407 | 58 |
| Wuhan Shanhai Zhihe Biotechnology Co., Ltd. | 17771424646 | shoubull@126.com | China | 985 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24989 | 58 |
| Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 18100677375 | sales@szzxbio.com | China | 3000 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5840 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D co.,Ltd. | 025-025-66113011 18626450290 | cb5@aikonchem.com | China | 10358 | 58 |
