Cat. No.: HY-155005

EGFR mutant-IN-2

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Based on 1 Customer Validation

EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR^{L858R/T790M/C797S} mutant with an IC₅₀ value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR^{del19/T790M/C797S} mutant with an IC₅₀ value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity.

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

Purity: 97.0%
CAS No.: 2770009-06-6
Formula: C₂₇H₂₇F₃N₆O₂S
Molecular Weight:556.60

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

EGFR mutant-IN-2 Chemical Structure

CAS No.: 2770009-06-6

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Antibody-Drug Conjugates

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	22.6 μM Compound: D51	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
BaF3	IC₅₀	0.026 μM Compound: D51	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
BaF3	IC₅₀	0.641 μM Compound: D51	Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
NCI-H1975	IC₅₀	0.096 μM Compound: D51	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
PC-9	IC₅₀	0.05 μM Compound: D51	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]

Chemical Information

CAS No. 2770009-06-6
Appearance Solid
Molecular Weight 556.60
Formula C₂₇H₂₇F₃N₆O₂S
Color Light yellow to yellow
SMILES

FC(F)(F)C1=CN=C(NC2=CC(C=CN3CCN(C)C)=C3C=C2)N=C1C4=CN(S(CC)(=O)=O)C5=C4C=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (224.58 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7966 mL

8.9831 mL

17.9662 mL

5 mM

0.3593 mL

1.7966 mL

3.5932 mL

10 mM

0.1797 mL

0.8983 mL

1.7966 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Dong H, et al. Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC. J Med Chem. 2023 May 25;66(10):6849-6868. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7966 mL	8.9831 mL	17.9662 mL	44.9156 mL
	5 mM	0.3593 mL	1.7966 mL	3.5932 mL	8.9831 mL
	10 mM	0.1797 mL	0.8983 mL	1.7966 mL	4.4916 mL
	15 mM	0.1198 mL	0.5989 mL	1.1977 mL	2.9944 mL
	20 mM	0.0898 mL	0.4492 mL	0.8983 mL	2.2458 mL
	25 mM	0.0719 mL	0.3593 mL	0.7186 mL	1.7966 mL
	30 mM	0.0599 mL	0.2994 mL	0.5989 mL	1.4972 mL
	40 mM	0.0449 mL	0.2246 mL	0.4492 mL	1.1229 mL
	50 mM	0.0359 mL	0.1797 mL	0.3593 mL	0.8983 mL
	60 mM	0.0299 mL	0.1497 mL	0.2994 mL	0.7486 mL
	80 mM	0.0225 mL	0.1123 mL	0.2246 mL	0.5614 mL
	100 mM	0.0180 mL	0.0898 mL	0.1797 mL	0.4492 mL

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EGFR mutant-IN-2

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

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

EGFR mutant-IN-2

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

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

EGFR mutant-IN-2 Related Classifications

HY-155005 Related Classifications