Name: LC-2
Brand: Selleck Chemicals
SKU: S6996
Rating: 5 (1 reviews)

LC-2 is a first PROTAC capable of degrading endogenous KRAS^G12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRAS^G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS^G12C degradation leading to suppression of MAPK signaling.

LC-2 Chemical Structure

CAS: 2502156-03-6

Purity & Quality Control

Batch: S699601 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.58%

99.58

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Signaling Pathway

Ras Signaling Pathway

Choose Selective Ras Inhibitors

Biological Activity

Description

LC-2 is a first PROTAC capable of degrading endogenous KRAS^G12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRAS^G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS^G12C degradation leading to suppression of MAPK signaling.

Targets

KRAS G12C ^[1]

References

[1] Michael J Bond, et al. ACS Cent Sci. 2020 Aug 26;6(8):1367-1375.

Chemical Information & Solubility

Molecular Weight	1132.78	Formula	C₅₉H₇₁ClFN₁₁O₇S
CAS No.	2502156-03-6	SDF	--
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (88.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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