Synonym
GW6604; GW-6604; GW 6604;
IUPAC/Chemical Name
2-phenyl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine
InChi Key
BDCBRQYHYNUWAM-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H14N4/c1-2-6-14(7-3-1)18-12-15(9-11-21-18)16-13-22-23-19(16)17-8-4-5-10-20-17/h1-13H,(H,22,23)
SMILES Code
C1(C2=CC=CC=C2)=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.
In vitro activity:
As shown in Figure 2c, GW6604 inhibited ALK5 activity with an IC50 of 140 nm, a potency comparable to that measured in an ALK5 binding assay (IC50=107 nm (Table 1).
Reference: Br J Pharmacol. 2005 May;145(2):166-77. https://pubmed.ncbi.nlm.nih.gov/15723089/
In vivo activity:
Treatment with GW6604 induced a 4.7-fold increase in hepatocyte proliferation in partially hepatectomized TGF-β transgenic mice (1.8±0.4 and 8.5±2.2 stained nuclei per field in animals treated with vehicle and GW6604, respectively, P=0.02 (t-test)) (Figure 3).
Reference: Br J Pharmacol. 2005 May;145(2):166-77. https://pubmed.ncbi.nlm.nih.gov/15723089/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
298.35
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, Loriolle F, Gauthier JM, Papworth SA, Laroze A, Gellibert F, Huet S. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. doi: 10.1038/sj.bjp.0706172. PMID: 15723089; PMCID: PMC1576127.
In vitro protocol:
1. de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, Loriolle F, Gauthier JM, Papworth SA, Laroze A, Gellibert F, Huet S. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. doi: 10.1038/sj.bjp.0706172. PMID: 15723089; PMCID: PMC1576127.
In vivo protocol:
1. de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, Loriolle F, Gauthier JM, Papworth SA, Laroze A, Gellibert F, Huet S. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. doi: 10.1038/sj.bjp.0706172. PMID: 15723089; PMCID: PMC1576127.
1: Ciayadi R, Kelso GF, Potdar MK, Harris SJ, Walton KL, Harrison CA, Hearn MT. Identification of protein binding partners of ALK-5 kinase inhibitors. Bioorg Med Chem. 2013 Nov 1;21(21):6496-500. doi: 10.1016/j.bmc.2013.08.038. Epub 2013 Aug 29. PubMed PMID: 24055074.
2: de Gouville AC, Huet S. Inhibition of ALK5 as a new approach to treat liver fibrotic diseases. Drug News Perspect. 2006 Mar;19(2):85-90. Review. PubMed PMID: 16628263.
3: de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, Loriolle F, Gauthier JM, Papworth SA, Laroze A, Gellibert F, Huet S. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. PubMed PMID: 15723089; PubMed Central PMCID: PMC1576127.
