ChemicalBook > CAS DataBase List > ERK5-IN-2

ERK5-IN-2

Product Name
ERK5-IN-2
CAS No.
1888305-96-1
Chemical Name
ERK5-IN-2
Synonyms
ERK5-IN-2;ERK5 inhibitor 2;ERK5-IN-2 ，S6786;ERK5-IN-2, 10 mM in DMSO;ERK5-IN 2; ERK5 IN-2; ERK5-IN-2;1H-Pyrrole-2-carboxamide, 4-(2-bromo-6-fluorobenzoyl)-N-3-pyridinyl-;4-(2-Bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide;Inhibitor,ERK5 IN 2,Extracellular signal regulated kinases,inhibit,ERK,ERK-5-IN-2,ERK5IN2
CBNumber
CB95430841
Molecular Formula
C17H11BrFN3O2
Formula Weight
388.19
MOL File
1888305-96-1.mol
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ERK5-IN-2 Property

Boiling point:
525.1±50.0 °C(Predicted)
Density 
1.628±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: 250 mg/mL (644.01 mM)
pka
12.92±0.50(Predicted)
form 
Solid
color 
White to off-white
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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.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0099026
Product name
ERK5-IN-2
Purity
98.67%
Packaging
5mg
Price
$150
Updated
2021/12/16
ChemScene
Product number
CS-0099026
Product name
ERK5-IN-2
Purity
98.67%
Packaging
10mg
Price
$250
Updated
2021/12/16
ChemScene
Product number
CS-0099026
Product name
ERK5-IN-2
Purity
98.67%
Packaging
25mg
Price
$500
Updated
2021/12/16
ChemScene
Product number
CS-0099026
Product name
ERK5-IN-2
Purity
98.67%
Packaging
50mg
Price
$850
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611948
Product name
ERK5-IN-2
Purity
>98%
Packaging
100mg
Price
$912.9
Updated
2021/12/16
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ERK5-IN-2 Chemical Properties,Usage,Production

Uses

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis[1].

in vivo

ERK5-IN-2 (compound 46) (p.o.; 100 mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin[1].
ERK5-IN-2 (i.v. or p.o.; 10 mg/kg for 0.083-24 hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2 cell permeability assay in both human and mouse[1].

Animal Model:Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts[1]
Dosage:100?mg/kg
Administration:P.o.; twice-daily; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days
Result:Tumor volumes were significantly reduced.
Animal Model:Female CD1 mice at 8-10 weeks of age[1]
Dosage:10 mg/kg
Administration:I.v. or p.o.; 0.083-24?hours
Result:The terminal plasma half-life was 38?min, with a plasma clearance of 27?mL/min/kg, and oral bioavailability of 68%.

IC 50

ERK5: 0.82 μM (IC50); ERK5 MEF2D: 3 μM (IC50)

References

[1] Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543. DOI:10.1016/j.ejmech.2019.05.057

ERK5-IN-2 Preparation Products And Raw materials

Raw materials

Preparation Products

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ERK5-IN-2 Suppliers

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1888305-96-1, ERK5-IN-2Related Search:


  • ERK5-IN 2; ERK5 IN-2; ERK5-IN-2
  • ERK5-IN-2
  • ERK5 inhibitor 2
  • 1H-Pyrrole-2-carboxamide, 4-(2-bromo-6-fluorobenzoyl)-N-3-pyridinyl-
  • 4-(2-Bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide
  • Inhibitor,ERK5 IN 2,Extracellular signal regulated kinases,inhibit,ERK,ERK-5-IN-2,ERK5IN2
  • ERK5-IN-2, 10 mM in DMSO
  • ERK5-IN-2 ，S6786
  • 1888305-96-1