FRAX486
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407180

CAS#: 1232030-35-1

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.


Chemical Structure

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FRAX486
CAS# 1232030-35-1

Theoretical Analysis

MedKoo Cat#: 407180
Name: FRAX486
CAS#: 1232030-35-1
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

Price and Availability

Size Price Availability Quantity
100.0mg USD 1650.0 2 Weeks
200.0mg USD 2250.0 2 Weeks
500.0mg USD 2950.0 2 Weeks
1.0g USD 3750.0 2 Weeks
2.0g USD 5250.0 2 Weeks
5.0g USD 9450.0 2 Weeks
Bulk inquiry

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

Preparing Stock Solutions

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.

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

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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.

FRAX486

100.0mg / USD 1650.0