WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407180
Description: FRAX486 is a potent p21-activated kinase (PAK) inhibitor (IC50 values are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively). FRAX486 rescues seizures and behavioral abnormalities such as hyperactivity and repetitive movements, thereby supporting the hypothesis that a drug treatment that reverses the spine abnormalities can also treat neurological and behavioral symptoms. A single administration of FRAX486 is sufficient to rescue all of these phenotypes in adult Fmr1 KO mice, demonstrating the potential for rapid, postdiagnostic therapy in adults with FXS. FRAX486 ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence.
MedKoo Cat#: 407180
Chemical Formula: C25H23Cl2FN6O
Exact Mass: 512.12944
Molecular Weight: 513.4
Elemental Analysis: C, 58.49; H, 4.52; Cl, 13.81; F, 3.70; N, 16.37; O, 3.12
Synonym: FRAX486; FRAX-486; FRAX 486.
IUPAC/Chemical Name: 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
InChi Key: DHKFOIHIUYFSOF-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H23Cl2FN6O/c1-2-34-23-15(11-19(24(34)35)18-5-3-16(26)12-20(18)27)14-30-25(32-23)31-17-4-6-22(21(28)13-17)33-9-7-29-8-10-33/h3-6,11-14,29H,2,7-10H2,1H3,(H,30,31,32)
SMILES Code: O=C1C(C2=CC=C(Cl)C=C2Cl)=CC3=CN=C(NC4=CC=C(N5CCNCC5)C(F)=C4)N=C3N1CC
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 513.4 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: Hayashi-Takagi A, Araki Y, Nakamura M, Vollrath B, Duron SG, Yan Z, Kasai H,
Huganir RL, Campbell DA, Sawa A. PAKs inhibitors ameliorate
schizophrenia-associated dendritic spine deterioration in vitro and in vivo
during late adolescence. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6.
doi: 10.1073/pnas.1321109111. Epub 2014 Apr 3. PubMed PMID: 24706880; PubMed
Central PMCID: PMC4035976.
2: Dolan BM, Duron SG, Campbell DA, Vollrath B, Shankaranarayana Rao BS, Ko HY,
Lin GG, Govindarajan A, Choi SY, Tonegawa S. Rescue of fragile X syndrome
phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc Natl
Acad Sci U S A. 2013 Apr 2;110(14):5671-6. doi: 10.1073/pnas.1219383110. Epub
2013 Mar 18. PubMed PMID: 23509247; PubMed Central PMCID: PMC3619302.