Cat. No.: HY-19815

Olafertinib

(Synonyms: CK-101; RX518)

Customer Review

Based on 1 Customer Validation

Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies.

For research use only. We do not sell to patients.

Purity: 99.51%
CAS No.: 1660963-42-7
Formula: C₂₉H₂₈F₂N₆O₂
Molecular Weight:530.57

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Olafertinib Chemical Structure

CAS No.: 1660963-42-7

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Sample (0.1mg)

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(In Japan)

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

GI50: 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19), 689 nM (EGFR WT)^[1].

All EGFR Isoforms :

In Vitro

Olafertinib (Compound CK-101) (72 h) selectively inhibits cell proliferation of cell lines expressing both the activating (e.g. HCC827, IC₅₀ < 0.015 μM) and resistance mutations (NCI-H1975, IC₅₀ < 0.005 μM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Olafertinib (Compound CK-101) (p.o., daily for 14 or 21 days) significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft mice models^[2].
Olafertinib inhibits tumor growth by up to 90% in a xenograft study of PC-9 cells in SCID/Beige mice^[2].
Olafertinib inhibits tumor growth by up to 95% in a xenograft study of NCI-H1975 cells in BALB/c nude mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1660963-42-7
Appearance Solid
Molecular Weight 530.57
Formula C₂₉H₂₈F₂N₆O₂
Color Light yellow to yellow
SMILES

OCCN1CCN(C2=C(F)C(F)=C(NC3=NC=C4C(C(C5=CC(NC(C=C)=O)=CC=C5)=CC=C4)=N3)C=C2)CC1
Synonyms

CK-101; RX518
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (235.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8848 mL

9.4238 mL

18.8477 mL

5 mM

0.3770 mL

1.8848 mL

3.7695 mL

10 mM

0.1885 mL

0.9424 mL

1.8848 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Johnson, M. et al., (2018) OA02.05 CK-101 (RX518), a Third Generation Mutant-Selective Inhibitor of EGFR in NSCLC: Results of an Ongoing Phase I/II Trial. Journal of Thoracic Oncology, Volume 13, Issue 10, S323.

[2]. Xiangping Qian, et al., Abstract 2078: CK-101 (RX518), a mutant-selective inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Res 1 July 2017; 77 (13_Supplement): 2078.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8848 mL	9.4238 mL	18.8477 mL	47.1191 mL
	5 mM	0.3770 mL	1.8848 mL	3.7695 mL	9.4238 mL
	10 mM	0.1885 mL	0.9424 mL	1.8848 mL	4.7119 mL
	15 mM	0.1257 mL	0.6283 mL	1.2565 mL	3.1413 mL
	20 mM	0.0942 mL	0.4712 mL	0.9424 mL	2.3560 mL
	25 mM	0.0754 mL	0.3770 mL	0.7539 mL	1.8848 mL
	30 mM	0.0628 mL	0.3141 mL	0.6283 mL	1.5706 mL
	40 mM	0.0471 mL	0.2356 mL	0.4712 mL	1.1780 mL
	50 mM	0.0377 mL	0.1885 mL	0.3770 mL	0.9424 mL
	60 mM	0.0314 mL	0.1571 mL	0.3141 mL	0.7853 mL
	80 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5890 mL
	100 mM	0.0188 mL	0.0942 mL	0.1885 mL	0.4712 mL

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Olafertinib

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

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MCE Bioactive Compound Library

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Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Olafertinib Related Classifications

Cat. No.: HY-19815