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Olafertinib

Name: Olafertinib
Brand: TargetMol
SKU: TQ0255
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. TQ0255Cas No. 1660963-42-7

Alias RX-518, EGFR-IN-3, CK-101

Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.

Olafertinib

🥰Excellent

Purity: 99.70%

Catalog No. TQ0255Alias RX-518, EGFR-IN-3, CK-101Cas No. 1660963-42-7

Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$41	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$155	In Stock	In Stock
25 mg	$322	In Stock	In Stock
50 mg	$472	In Stock	In Stock
100 mg	$693	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$113	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.70%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.
Targets&IC50	EGFR (del19):10 nM (GI50), EGFR (L858R/T790M):5 nM (GI50), EGFR (WT):689 nM (GI50)
In vitro	CK-101 specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR. It selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM).
In vivo	CK-101 significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in the WT EGFR tumor xenograft model.
Synonyms	RX-518, EGFR-IN-3, CK-101

Chemical Properties

Molecular Weight	530.57
Formula	C₂₉H₂₈F₂N₆O₂
Cas No.	1660963-42-7
Smiles	OCCN1CCN(CC1)c1ccc(Nc2ncc3cccc(-c4cccc(NC(=O)C=C)c4)c3n2)c(F)c1F
Relative Density.	1.350 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store 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

H2O: Insoluble

DMSO: 120 mg/mL (226.17 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.54 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8848 mL	9.4238 mL	18.8477 mL	94.2383 mL
5 mM	0.3770 mL	1.8848 mL	3.7695 mL	18.8477 mL
10 mM	0.1885 mL	0.9424 mL	1.8848 mL	9.4238 mL
20 mM	0.0942 mL	0.4712 mL	0.9424 mL	4.7119 mL
50 mM	0.0377 mL	0.1885 mL	0.3770 mL	1.8848 mL
100 mM	0.0188 mL	0.0942 mL	0.1885 mL	0.9424 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc