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商品描述
APS-2-79
- Catalog No.：MC1342
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 2002381-25-9
- MolecularFormula：
- C23H21N3O3
- Purity：
- >98%
- Target：
- ERK
- IC50：
- No data
- In Vitro：
- APS-2-79 inhibits BRAF and CRAF phosphorylation of MEK in a KSR-dependent manner. APS-2-79 does not affect BRAF(V600E)-induced MAPK activation in cells. APS-2-79 impedes KSR-stimulated MAPK signalling within cells through wild-type and MEK equally. APS-2-79 synergizes with trametinib specifically in Ras-mutant cells compared to the HER-family and SRC-family inhibitors lapatinib and sarcatinib. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. The IC50 value of APS-2-79 against ATPbiotin probe-labelling of KSR2 is 120 nM[1].
- Fields：
- APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
- Specificity：
- Target: ERK. Fields: APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
- Source：
- Rabbit
- Dilution：
- WB 1:500-2000
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- APS 2 79,APS279,APS-279
- MolecularWeight(Da)：
- 387.16
- References：
- [1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116.
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