G-5555 manufacturers
- G-5555
-
- $48.00 / 1mg
-
2025-05-26
- CAS:1648863-90-4
- Min. Order:
- Purity: 99.76%
- Supply Ability: 10g
- G-5555
-
- $48.00 / 1mg
-
2025-05-26
- CAS:1648863-90-4
- Min. Order:
- Purity: 99.76%
- Supply Ability: 10g
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| Product Name: | G-5555 | | Synonyms: | 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 | | CAS: | 1648863-90-4 | | MF: | C25H25ClN6O3 | | MW: | 492.96 | | EINECS: | | | Product Categories: | | | Mol File: | 1648863-90-4.mol |  |
| | G-5555 Chemical Properties |
| 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 |
| | G-5555 Usage And Synthesis |
| 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 |
| | G-5555 Preparation Products And Raw materials |
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