WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407183
Description: GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.
MedKoo Cat#: 407183
Chemical Formula: C31H30FN7O
Exact Mass: 535.24959
Molecular Weight: 535.63
Elemental Analysis: C, 69.51; H, 5.65; F, 3.55; N, 18.31; O, 2.99
Synonym: GNF-8625; GNF 8625; GNF8625.
IUPAC/Chemical Name: (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-HHHXNRCGSA-N
InChi Code: 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/t27-/m1/s1
SMILES Code: OC1CCN(C2=NC=CC(C3=NC(C4=CN=C5C=CC(N6[C@@H](C7=CC=CC(F)=C7)CCC6)=NN54)=CC=C3)=C2)CC1
Appearance: Solid powder
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
The following data is based on the product molecular weight 535.63 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|
1: Choi HS, Rucker PV, Wang Z, Fan Y, Albaugh P, Chopiuk G, Gessier F, Sun F,
Adrian F, Liu G, Hood T, Li N, Jia Y, Che J, McCormack S, Li A, Li J, Steffy A,
Culazzo A, Tompkins C, Phung V, Kreusch A, Lu M, Hu B, Chaudhary A, Prashad M,
Tuntland T, Liu B, Harris J, Seidel HM, Loren J, Molteni V.
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and
Selective Pan-TRK Inhibitors. ACS Med Chem Lett. 2015 Mar 16;6(5):562-7. doi:
10.1021/acsmedchemlett.5b00050. eCollection 2015 May 14. PubMed PMID: 26005534;
PubMed Central PMCID: PMC4434478.