9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl-
![9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- Structure](CAS/20210111/GIF/2463200-44-2.gif)
- CAS No.
- 2463200-44-2
- Chemical Name:
- 9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl-
- Synonyms
- RXN00442;EGFR-IN-11;9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl-
- CBNumber:
- CB78186367
- Molecular Formula:
- C29H35N9O2S
- Molecular Weight:
- 573.71
- MDL Number:
- MOL File:
- 2463200-44-2.mol
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- Properties
| Boiling point | 808.3±75.0 °C(Predicted) |
|---|---|
| Density | 1.48±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO : 125 mg/mL (217.88 mM; Need ultrasonic) |
| pka | 7.88±0.42(Predicted) |
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- price
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- Chemical Properties,Uses,Production
Biological Activity
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1]. EGFR-IN-11 (Compound D9; 0.0001-10 μM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 μM, respectively[1]. EGFR-IN-11 (0.01-1.00 μM for HCC827 cells; 0.1-10.00 μM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1]. EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells.[1]EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell[1].
References
[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- Preparation Products And Raw materials
Raw materials
Preparation Products
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32715 | 60 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9824 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24018 | 58 |
| Shanghai Yiyan Biotechnology Co. , Ltd. | 021-69985186 13611928337 | 3427709316@qq.com | China | 7984 | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 5019 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9180 | 58 |