EGFR-IN-44

Name: EGFR-IN-44
Brand: MedChemExpress
SKU: HY-145844

Cat. No.: HY-145844: FAQs
Data Sheet Handling Instructions

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EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers.

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

EGFR-IN-44 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC₅₀: 0.26 nM (EGFR T790M/L858R), 1.33 nM (EGFR L858R), 4.11 nM (EGFR)^[1]

In Vitro

EGFR-IN-44 (Compound 6a) (0-10 µM, 72 h) shows anti-proliferative activities against tumor cell lines^[1].
EGFR-IN-44 binds to the ATP binding site of EGFR^[1].
EGFR-IN-44 (0-10 nM, 48 h) induces H1975 cell apoptosis via the mitochondrial pathway, arrests cell cycle in G0/G1 phase, and suppresses cell migration^[1].
EGFR-IN-44 (0-10 nM, 48 and 72h) shows hypotoxicity against normal cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	H1975 (EGFR^T790M/L858R), PC9 (EGFR^del19), and H292 (EGFR^WT)
Concentration:	0-10 µM
Incubation Time:	72 h
Result:	Showed anti-proliferative activities with IC₅₀ values of 0.0022 ± 0.001, 0.0048 ± 0.001, and 4.499 ± 0.057 µM against H1975, PC9, and H292 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:	H1975
Concentration:	1, 5, and 10 nM
Incubation Time:	48 h
Result:	Effectively induced cell apoptosis in a dose-dependent manner. Resulted in 33.7%, 52.4%, and 56.2% apoptosis at 1, 5, and 10 µM, respectively, compared to 5.81% apoptosis in the control group.

Western Blot Analysis^[1]

Cell Line:	H1975
Concentration:	5, 10, and 25 nM
Incubation Time:	48 h and 72 h
Result:	Dose-dependently upregulated the expression levels of the proapoptotic proteins Bad and Bax and downregulated the expression level of the antiapoptotic protein Bcl-2. Sufficiently reduced the phosphorylation of EGFR and AKT.

Cell Cycle Analysis^[1]

Cell Line:	H1975
Concentration:	5 nM
Incubation Time:	0, 12, 24, or 48 h
Result:	Exhibited a significant increase in the G0/G1 cell population and a dramatic decrease in G2/M phase.

Cell Cytotoxicity Assay^[1]

Cell Line:	LO2, HK2, HLF, and 293A
Concentration:	0.1, 1, 5, and 10 µM
Incubation Time:	48 h and 72 h
Result:	Showed hypotoxicity with IC₅₀ values of 7.247, 4.586, 3.787, and 2.925 µM against LO2, HK2, HLF, and 293A cells, respectively. The cell morphology was changed compared to the control.

In Vivo

EGFR-IN-44 (Compound 6a) (25 mg/kg; i.g.; daily, 7days) shows strong antitumor activity without obvious toxicity^[1].

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

Animal Model:	Male BALB/c nude mice (5 weeks old, 18 - 20 g), H1975 xenograft model^[1]
Dosage:	25 mg/kg
Administration:	Intragastric administration, daily, 7 days
Result:	Showed strong tumor inhibition (TGI = 90.24%) without obvious toxicity.

Animal Model:

Male Sprague–Dawley (SD) rats^[1]

Dosage:

1 mg/kg and 5 mg/kg

Administration:

Intravenous injection and oral administration (Pharmacokinetic Analysis)

Result:

In Vivo PK parameters of EGFR-IN-44 ^[1]

Parameters Dose(mg/kg)	EGFR-IN-44 5 (po)	1 (iv)
t_1/2 (h)	8.60 ± 1.8	1.42 ± 0.1
T_max (h)	4.00 ± 0.002	/
C_max (ng/mL)	80.40 ± 2.7	/
Vz _{F_pred} (L/kg)	220.80 ± 41.2	6.83 ± 08
AUC_0-t (H.ng/mL)	490.41 ± 29.9	291.91 ± 38.2
AUC_0-∞ (H.ng/mL)	491.02 ± 44.2	295.76 ± 38.8
MRT_0-last (h)	7.93 ± 0.8	1.35 ± 01
CL (mL/h/kg)	17.79 ± 3.9	3.12 ± 0.4
F(%)	33.57 ± 5.9	/

F = (AUC_0-inf-PO × DOSE_IV)/(AUC_0-inf-IV × DOSE _PO)*100%.

Molecular Weight

537.08

Formula

C₂₇H₂₉ClN₆O₂S

SMILES

C=CC(NC1=CC(NC2=NC(C3=CSC4=CC=CC=C43)=C(C=N2)Cl)=C(C=C1N(CCN(C)C)C)OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Baijiao An, et al. Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. Bioorg Chem. 2022 May;122:105743. [Content Brief]

EGFR-IN-44 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-44EGFRApoptosisEpidermal growth factor receptorErbB-1HER1H1975AKTBcl-2BaxBadBALB/c nude micenon-small-cell lung cancers NSCLCInhibitorinhibitorinhibit

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