ARRY-614
- Product Name
- 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
- Formula Weight
- 556.63
- MOL File
- 945614-12-0.mol
ARRY-614 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 26187
- Product name
- Pexmetinib
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 26187
- Product name
- Pexmetinib
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 26187
- Product name
- Pexmetinib
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- P293620
- Product name
- Pexmetinib
- Packaging
- 100mg
- Price
- $900
- Updated
- 2021/12/16
- Product number
- P293620
- Product name
- Pexmetinib
- Packaging
- 5mg
- Price
- $135
- Updated
- 2021/12/16
ARRY-614 Chemical Properties,Usage,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
ARRY-614 Suppliers
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View Lastest Price from ARRY-614 manufacturers
- Product
- Pexmetinib 945614-12-0
- Price
- US $1.00/KG
- Min. Order
- 1g
- Purity
- Min98% HPLC
- Supply Ability
- g/kg /ton
- Release date
- 2019-12-20