MedKoo Cat#: 407180 | Name: FRAX486
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

FRAX486
FRAX486
CAS#1232030-35-1

Theoretical Analysis

MedKoo Cat#: 407180

Name: FRAX486

CAS#: 1232030-35-1

Chemical Formula: C25H23Cl2FN6O

Exact Mass: 512.1294

Molecular Weight: 513.40

Elemental Analysis: C, 58.49; H, 4.52; Cl, 13.81; F, 3.70; N, 16.37; O, 3.12

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 3,250.00 2 Weeks
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Related CAS #
No Data
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 513.40 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.

Recalculate based on batch purity %
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.