GNE-8525

 CAS No.: 1196546-33-4  Cat No.: BP-300132  Purity: 98%  HPLC  HNMR  MS 4.5  

This active molecular is a selective pan-TRK inhibitor. GNE-8525 shows potent antiproliferation activity (IC50 = 0.003 μM) and it shows in vivo antitumor efficacy in tumor xenograft model derived from the KM12 cell line. TRKA are believed to be the key oncogenic driver in many tumors including glioblastoma, melanoma and so on.

GNE-8525

Structure of 1196546-33-4

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Ligand for Target Protein
Molecular Formula
C31H30FN7O
Molecular Weight
535.63
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Powder

* For research and manufacturing use only. Not for human or clinical use.

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50 mg $838 In stock

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Purity
98%
Solubility
Soluble in DMSO
Appearance
Powder
Application
antitumor
ShelfLife
2 month in rt, long time
Storage
-20°C Freezer
IUPACName
1-[4-[6-[6-[2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]pyridin-2-yl]piperidin-4-ol
Synonyms
GNF-8625; GNF 8625; GNF8625. (R)-1-(6-(6-(2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)-[2,4'-bipyridin]-2'-yl)piperidin-4-ol
InChI Key
BLGCSOKKBWHJMB-UHFFFAOYSA-N
InChI
InChI=1S/C31H30FN7O/c32-23-5-1-4-22(18-23)27-8-3-15-38(27)30-10-9-29-34-20-28(39(29)36-30)26-7-2-6-25(35-26)21-11-14-33-31(19-21)37-16-12-24(40)13-17-37/h1-2,4-7,9-11,14,18-20,24,27,40H,3,8,12-13,15-17H2
Canonical SMILES
C1CC(N(C1)C2=NN3C(=NC=C3C4=CC=CC(=N4)C5=CC(=NC=C5)N6CCC(CC6)O)C=C2)C7=CC(=CC=C7)F

What is the pharmacokinetics of GNE-8525?

GNE-8525 exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration.

27/1/2016

What is the activity of GNE-8525 in vitro?

GNE-8525 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC50 values of >5000 nM, >5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively.

20/6/2016

GNE-8525 suppresse CYP-induced nociceptive behavior?

GNE-8525 suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice.

6/12/2018

suppresses CYP-induced edema and hemorrhage

GNE-8525 do well in suppressing CYP-induced edema and hemorrhage in mouse bladder. Very useful for our study!

8/1/2019

display concentration-dependent protection of neurons from degeneration

GNE-8525 displays concentration-dependent protection of neurons from degeneration in vitro. Satisfied with product.

21/12/2021

Stock concentration: *
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L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g

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