ChemicalBook > CAS DataBase List > G-5555

G-5555

Product Name
G-5555
CAS No.
1648863-90-4
Chemical Name
G-5555
Synonyms
G-5555;G5555;G 5555;G-5555, 10 mM in DMSO;PAK1 inhibitor (g-5555);p21 activated kinases,G-5555,PAK,Inhibitor,G 5555,inhibit,G5555;8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(met;8-((trans-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one;8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one;Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-
CBNumber
CB33126700
Molecular Formula
C25H25ClN6O3
Formula Weight
492.96
MOL File
1648863-90-4.mol
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G-5555 Property

Boiling point:
684.6±65.0 °C(Predicted)
Density 
1.363±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml
form 
A crystalline solid
pka
6.86±0.40(Predicted)
color 
White to light yellow
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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

Sigma-Aldrich
Product number
SML3237
Product name
G-5555
Purity
≥98% (HPLC)
Packaging
5MG
Price
$102.38
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3237
Product name
G-5555
Purity
≥98% (HPLC)
Packaging
25MG
Price
$431
Updated
2025/07/31
Cayman Chemical
Product number
21469
Product name
G-5555
Purity
≥98%
Packaging
500μg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
21469
Product name
G-5555
Purity
≥98%
Packaging
1mg
Price
$79
Updated
2024/03/01
Cayman Chemical
Product number
21469
Product name
G-5555
Purity
≥98%
Packaging
5mg
Price
$330
Updated
2024/03/01
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G-5555 Chemical Properties,Usage,Production

Description

G-5555 is an inhibitor of p21-activated kinase 1 (PAK1; Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis. It is selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% with IC50 values ranging from 9 to 52 nM. G-5555 inhibits phosphorylation of MEK, a downstream target of PAK1, in EBC1 cells (IC50 = 69 nM). G-5555 (10, 20, and 30 mg/kg) dose-dependently reduces phosphorylation of MEK in tumors from an H292 non-small cell lung cancer (NSCLC) mouse xenograft model. G-5555 inhibits hERG channels less than 50% at a concentration of 10 μM, indicating the potential for a low risk of QT interval prolongation and potentially fatal arrhythmias.

Uses

G 5555 is a high affinity group 1 p21-activated kinases (PAK) inhibitor.

in vivo

G-5555 exhibits low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM h) and high oral bioavailability (F = 80%) are achieved[1]. In an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice, G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298 and, when administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model and a PAK1 amplified breast cancer xenograft model, MDAMB-175[2].

IC 50

PAK1: 3.7 nM (Ki); PAK2: 11 nM (Ki)

storage

Store at -20°C

References

[1] CHUDI O. NDUBAKU*. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety[J]. ACS Medicinal Chemistry Letters, 2015, 6 12: 1241-1246. DOI: 10.1021/acsmedchemlett.5b00398
[2] RODOLPHO C BRAGA. Tuning HERG out: antitarget QSAR models for drug development.[J]. Current topics in medicinal chemistry, 2014: 1399-1415. DOI: 10.2174/1568026614666140506124442

G-5555 Preparation Products And Raw materials

Raw materials

Preparation Products

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G-5555 Suppliers

China 32 United Kingdom 1 United States 9 Global 42
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1648863-90-4, G-5555Related Search:


  • G-5555
  • 8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(met
  • G5555;G 5555
  • 8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
  • Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-
  • PAK1 inhibitor (g-5555)
  • p21 activated kinases,G-5555,PAK,Inhibitor,G 5555,inhibit,G5555
  • 8-((trans-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one
  • G-5555, 10 mM in DMSO
  • 1648863-90-4
  • C25H25ClN6O3