Olverembatinib
|
|
Olverembatinib ??
- ?? ?
- 630.4±55.0 °C(Predicted)
- ??
- 1.39±0.1 g/cm3(Predicted)
- ?? ??
- Store at -20°C
- ???
- DMSO : ≥ 100 mg/mL (187.77 mM)
- ??? ??
- ??? ??
- ?? ?? (pKa)
- 9.04±0.40(Predicted)
- ??
- Off-white to yellow
??
Olverembatinib C??? ??, ??, ??
??
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively). It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.??
GZD824 is a orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Breakpoint Cluster Region-Abelson (Bcr-Abl) kinases. It is a COVID19-related research product.Synthesis
In a recent patent, the synthesis of olverembatinib began with a Sonogashira coupling reaction of commercially available alkyne 24.1 with pyridinium bromide 24.2 to afford ester 24.3 in 98% yield. The N-Boc group of carbonate 24.3 was cleaved by refluxing in a mixture of MeOH and water to afford pyrazole 24.4 in 91% yield. Finally, potassium tert-butoxide-mediated amide formation with aniline 24.5 afforded olverembatinib (24) in 88% yield.
target
BCR-ABLOlverembatinib ?? ?? ? ???
???
1H-Pyrazolo[3,4-b]pyridine, 5-[2-(trimethylsilyl)ethynyl]-
4-(4-?????????)-3-(????????)???
5-???-1H-???[3,4-B]???
4-b]pyridine
??3-????-4-???????
?? ??
Olverembatinib ?? ??
???( 122)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
product@chemlin.com.cn | CHINA | 3009 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 33024 | 60 |
| TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 |
sales@tianpharm.com | CHINA | 304 | 58 |
| Accela ChemBio Inc. | +1-858-6993322 |
info@accelachem.com | United States | 21193 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 |
marketing@targetmol.com | United States | 32467 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 |
laboratory@coreychem.com | China | 30224 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 |
sales@hzclap.com | CHINA | 6312 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 28675 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 |
shawn@hirisunpharm.com | CHINA | 9911 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 |
sales@invivochem.cn | United States | 6391 | 58 |