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PROTAC K-Ras Degrader-4

🥰Excellent
Catalog No. T206045Cas No. 2938169-99-2

PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.

PROTAC K-Ras Degrader-4

PROTAC K-Ras Degrader-4

🥰Excellent
Catalog No. T206045Cas No. 2938169-99-2
PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.
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Product Introduction

Bioactivity
Description
PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.
In vitro
PROTAC K-Ras Degrader-4 (0-1 μM, 5 days) was used to treat GP2d cell lines and was found to inhibit the expression of DUSP6 and the proliferation of GP2d cells with KRASG12D mutation. [1]
Chemical Properties
Molecular Weight989.22
FormulaC50H60N12O6S2
Cas No.2938169-99-2
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (80.87 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.0109 mL5.0545 mL10.1090 mL50.5449 mL
5 mM0.2022 mL1.0109 mL2.0218 mL10.1090 mL
10 mM0.1011 mL0.5054 mL1.0109 mL5.0545 mL
20 mM0.0505 mL0.2527 mL0.5054 mL2.5272 mL
50 mM0.0202 mL0.1011 mL0.2022 mL1.0109 mL

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Keywords

PROTACKRasDegrader4
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