ARRY-614
- CAS No.
- 945614-12-0
- Chemical Name:
- ARRY-614
- Synonyms
- ARRY-614;pexmetinib,ARRY-614;Autophagy,p38 MAPK,ARRY 614,Pexmetinib,Inhibitor,ARRY614,inhibit;N-(3-tert-Butyl-1-p-tolyl-1H-pyrazol-5-yl)-N'-[5-fluoro-2-[1-(2-hydroxyethyl)-1H-indazol-5-yloxy]benzyl]urea;1-(3-(tertbutyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)benzyl)urea;1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[[5-fluoro-2-[1-(2-hydroxyethyl)indazol-5-yl]oxyphenyl]methyl]urea;Urea, N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[[5-fluoro-2-[[1-(2-hydroxyethyl)-1H-indazol-5-yl]oxy]phenyl]methyl]-
- CBNumber:
- CB22725624
- Molecular Formula:
- C31H33FN6O3
- Molecular Weight:
- 556.63
- MDL Number:
- MFCD28502055
- MOL File:
- 945614-12-0.mol
- MSDS File:
- SDS
| Boiling point | 694.1±55.0 °C(Predicted) |
|---|---|
| Density | 1.28±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | insoluble in H2O; ≥107.6 mg/mL in DMSO; ≥113 mg/mL in EtOH |
| form | solid |
| pka | 13.00±0.46(Predicted) |
| FDA UNII | 3750D0U8B5 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
ARRY-614 price More Price(14)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 26187 | Pexmetinib | 945614-12-0 | 1mg | $37 | 2024-03-01 | Buy |
| Cayman Chemical | 26187 | Pexmetinib | 945614-12-0 | 10mg | $283 | 2024-03-01 | Buy |
| Cayman Chemical | 26187 | Pexmetinib | 945614-12-0 | 5mg | $151 | 2024-03-01 | Buy |
| TRC | P293620 | Pexmetinib | 945614-12-0 | 100mg | $900 | 2021-12-16 | Buy |
| TRC | P293620 | Pexmetinib | 945614-12-0 | 5mg | $135 | 2021-12-16 | Buy |
ARRY-614 Chemical Properties,Uses,Production
Uses
Pexmetinib is a potent and orally bioavailable dual p38 MAPK/Tie-2 inhibitor preventing tumor growth.
Biological Activity
pexmetinib (arry-614) is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (mapk), and tie2/tek receptor tyrosine kinase. the in vitro ic50 values of arr y-614 for both tie2 and p38 mitogen-activated protein kinase are 1000 ng/ml and 100 ng/ml, respectively [1, 2].p38 is a group of mitogen-activated protein kinases. mapks are activated by the dual phosphorylation of tyr and thr residues in the thr-xaa-tyr motif in subdomain viii. data indicated that p38 mapk may mediate signaling to the nucleus [3].arry-614 is active against mapk and tie2/tek receptor tyrosine kinase in cells. in primary human bone marrow stromal cells, arry-614 inhibited basal cytokines with an ic50 value ranging from 50-100 nm [4].in dose escalation or expansion cohorts, treatment with arry-614 either once daily or twice daily was applied to forty-five patients. arry-614 reduced the levels of circulating biomarkers and the p38 mapk activation of bone marrow [1]. in ex vivo stimulated human whole blood, lps-induced cytokines was inhibited by arry-614 with an ic50 value ranging from 50-120 nm. arry-614 inhibited the release of il-6 from sea- or lps-challenged mice with an ed50 value less than 10 mg/kg. combining arry-614 with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone [4].
References
[1]. garcia-manero g, khoury hj, jabbour e, et al. a phase i study of oral arry-614, a p38 mapk/tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes. clinical cancer research, 2015, 21(5): 985-994.
[2]. wollenberg la, corson dt, nugent ca, et al. an exploratory, randomized, parallel-group, open-label, relative bioavailability study with an additional two-period crossover food-effect study exploring the pharmacokinetics of two novel formulations of pexmetinib (arry-614). clinical pharmacology: advances and applications, 2015, 7: 87.
[3]. raingeaud j, whitmarsh aj, barrett t, et al. mkk3-and mkk6-regulated gene expression is mediated by the p38 mitogen-activated protein kinase signal transduction pathway. molecular and cellular biology, 1996, 16(3): 1247-1255.
[4]. winski s, humphries m, yeh t, et al. activity of arry-614, an inhibitor of p38 map kinase and angiogenic targets, in hematologic malignancies. cancer research, 2009, 69(9 supplement): 331-331.
ARRY-614 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4604 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
View Lastest Price from ARRY-614 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2019-12-23 | Pexmetinib
945614-12-0
|
US $1.00 / KG | 1g | Min98% HPLC | g/kg /ton | Career Henan Chemical Co |
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- Pexmetinib
945614-12-0
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co