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NSC228155 EGFR activator

Name: NSC228155
Brand: Selleck Chemicals
SKU: S8312
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S8312

NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.

Chemical Structure

Molecular Weight: 290.25

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.65%

99.65

Related Targets	VEGFR JAK PDGFR FGFR Src FLT3 HER2 Bcr-Abl HIF BTK ALK Syk FAK VDA
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Chemical Information, Storage & Stability

Molecular Weight	290.25	Formula	C₁₁H₆N₄O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	113104-25-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=[N+](C(=C1)SC2=CC=C(C3=NON=C23)[N+](=O)[O-])[O-]

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (34.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.63mg/ml (2.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.63mg/ml (2.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	EGFR ^[2] KIX-KID interaction ^[3] 0.36 μM
In vitro	NSC 228155 promotes transactivation of several RTKs, including ErbB2 and ErbB3, Insulin R and IGF-1 R receptors in the cells. It stimulates dimerization of sEGFR domain II^[1]. NSC 228155 can rapidly move across cell membranes and disperse within both cytoplasmic and nuclear compartments. It rapidly generates hydrogen peroxide within cells^[2]. NSC 228155 is also a potent inhibitor of KIX-KID interaction(IC50 = 0.36 μM), but it is not particularly selective against CREB-mediated gene transcription in HEK 293T cells^[3].
References	[1] https://pubmed.ncbi.nlm.nih.gov/24496106/ [2] https://pubmed.ncbi.nlm.nih.gov/26883293/ [3] https://pubmed.ncbi.nlm.nih.gov/23953193/

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