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2002381-31-7

APS-2-79 is an inhibitor of MAPK signaling dependent on kinase suppressor of Ras (KSR). It inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes, stabilizes KSR2 in an inactive state, and reduces interactions between B-RAF and KSR2-MEK1 complexes. APS-2-79 also enhances the efficacy of the MEK inhibitor trametinib, further reducing cell viability in certain cell lines.
Used in Pharmaceutical Industry:
APS-2-79 is used as a modulator of KSR-dependent MAPK signaling for antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and the activation of KSR-bound MEK. This makes it a potential therapeutic agent for targeting specific cancer cell lines with K-Ras mutations.
Used in Cancer Research:
APS-2-79 is used as an inhibitor of KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells. It enhances the efficacy of the MEK inhibitor trametinib, further reducing cell viability in HCT116 and A549 cell lines containing K-Ras mutations, but not B-RAF mutant SK-MEL-239 and A375 cell lines, when used at a concentration of 1 μM. This suggests its potential use in cancer research for developing targeted therapies against specific mutations.

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  • 2002381-31-7 Structure

  • Basic information

    1. Product Name: APS-2-79
    2. Synonyms: APS-2-79;APS-2-79 (hydrochloride)
    3. CAS NO:2002381-31-7
    4. Molecular Formula: C23H22ClN3O3
    5. Molecular Weight: 423.89208
    6. EINECS: -0
    7. Product Categories: N/A
    8. Mol File: 2002381-31-7.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: APS-2-79(CAS DataBase Reference)
    10. NIST Chemistry Reference: APS-2-79(2002381-31-7)
    11. EPA Substance Registry System: APS-2-79(2002381-31-7)

  • 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: 2002381-31-7(Hazardous Substances Data)

2002381-31-7 Usage

in vitro

aps-2-79 was found to be able to suppress ksr-stimulated mek and erk phosphorylation. this mapk signalling suppression caused by aps-2-79 was dependent on direct targeting of ksr as an active site mutant, which had been demonstrated to stimulate ksr-based mapk outputs independent of atp-binding, which could significantly diminish the activity of aps-2-79. moreover, the ksr-stimulated mek phosphorylation caused by raf was reduced by the addition of aps-2-79 markedly. in addition, aps-2-79 was no effetive when ksr was absent or when the ksr2(a690f) mutant was used for in vitro assays, indicating that the activity of aps-2-79 was from direct targeting of ksr. however, aps-2-79 was found to lack direct activity against the highly homologous active raf family kinases, such as recombinant braf and craf, or cellular braf(v600e) [1].

IC 50

120 nm

references

[1] dhawan ns, scopton ap, dar ac. small molecule stabilization of the ksr inactive state antagonizes oncogenic ras signalling. nature. 2016 sep 1;537(7618):112-116.

Check Digit Verification of cas no

The CAS Registry Mumber 2002381-31-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 2,0,0,2,3,8 and 1 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 2002381-31:
(9*2)+(8*0)+(7*0)+(6*2)+(5*3)+(4*8)+(3*1)+(2*3)+(1*1)=87
87 % 10 = 7
So 2002381-31-7 is a valid CAS Registry Number.

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