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FRAX1036 is a selective inhibitor of p21-activated kinase 1 (PAK1), a serine/threonine kinase that plays a crucial role in tumorigenesis. It is derived from the downstream signaling of Rac1 and Cdc42 and has demonstrated the ability to induce apoptosis in breast cancer cells. Furthermore, FRAX1036 has been shown to enhance the activity of the microtubule stabilizing agent, docetaxel, and disrupt PAK1 to inhibit oncogenic KRAS signaling in non-small cell lung cancer cells.

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  • 6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-{[2-(1-methylpiperidin-4-yl)ethyl]amino}pyrido[2,3-d]pyrimidin-7-one

    Cas No: 1432908-05-8

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  • 1432908-05-8 Structure
  • Basic information

    1. Product Name: FRAX1036
    2. Synonyms: FRAX1036;FRAX1036 (Free base)
    3. CAS NO:1432908-05-8
    4. Molecular Formula: C28H32ClN7O
    5. Molecular Weight: 518.05298
    6. EINECS: N/A
    7. Product Categories: N/A
    8. Mol File: 1432908-05-8.mol
  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: N/A
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: N/A
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: Soluble in DMSO
    9. CAS DataBase Reference: FRAX1036(CAS DataBase Reference)
    10. NIST Chemistry Reference: FRAX1036(1432908-05-8)
    11. EPA Substance Registry System: FRAX1036(1432908-05-8)
  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 1432908-05-8(Hazardous Substances Data)

1432908-05-8 Usage

Uses

Used in Pharmaceutical Industry:
FRAX1036 is used as an anticancer agent for targeting and inhibiting the activity of p21-activated kinase 1 (PAK1), which is involved in tumorigenesis. Its application in this context is due to its ability to induce apoptosis in breast cancer cells and potentiate the activity of docetaxel, a microtubule stabilizing agent.
Used in Oncology Research:
FRAX1036 is used as a research tool for studying the role of PAK1 in oncogenic KRAS signaling in non-small cell lung cancer cells. Its application in this field is based on its effectiveness in disrupting PAK1 and inhibiting the signaling pathways that contribute to cancer progression.
Used in Drug Development:
FRAX1036 is used as a potential therapeutic agent in the development of new cancer treatments. Its application in drug development is due to its ability to target PAK1, a key player in tumorigenesis, and its potential to enhance the efficacy of existing cancer treatments like docetaxel.

in vitro

previous study demonstrated that the administration of docetaxel with either frax1036 or pak1 small interfering rna oligonucleotides was able to alter signaling to cytoskeletal-associated proteins dramatically, such as stathmin, and also able to induce microtubule disorganization and cellular apoptosis. in addition, the live-cell imaging data showed that the duration of mitotic arrest mediated by docetaxel could be significantly reduced by the treatment of frax1036, which was associated with increased kinetics of apoptosis [1].

in vivo

in previous animal study, the untreated mice bearing kt21 transplants showed ventricular invasion, whereas ben-men grew at the injection site. efficacy results found that the treatment with frax1036 could lead to a slower tumor growth, with reduction in body mass index (bmi) signals of 37% when compared to vehicle cohort [2].

references

[1] ong cc et al. small molecule inhibition of group i p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. breast cancer res.2015 apr 23;17:59. [2] chow hy et al. group i paks as therapeutic targets in nf2-deficient meningioma. oncotarget.2015 feb 10;6(4):1981-94.

Check Digit Verification of cas no

The CAS Registry Mumber 1432908-05-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,3,2,9,0 and 8 respectively; the second part has 2 digits, 0 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1432908-05:
(9*1)+(8*4)+(7*3)+(6*2)+(5*9)+(4*0)+(3*8)+(2*0)+(1*5)=148
148 % 10 = 8
So 1432908-05-8 is a valid CAS Registry Number.

1432908-05-8Downstream Products

1432908-05-8Relevant articles and documents

An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036

Koval, Alexander B.,Wuest, William M.

, p. 449 - 451 (2016/01/12)

FRAX-1036 is a p21-activated kinase I inhibitor of significant interest to cancer biologists yet no commercial providers or detailed procedures are available. In this Letter, we chronicle the optimized synthesis of FRAX-1036, one of the most specific Pak1

PAK INHIBITORS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS

-

Paragraph 0617; 0640, (2013/05/21)

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders.

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