2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR/HER2/DHFR-IN-1

EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis.

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EGFR/HER2/DHFR-IN-1 Chemical Structure

EGFR/HER2/DHFR-IN-1 Chemical Structure

CAS No. : 2820126-37-0

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EGFR/HER2/DHFR-IN-1 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Description

EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis[1].

IC50 & Target

apoptosis; 0.153 μM (EGFR); 0.108 μM (HER2); 0.291 μM (DHFR)[1]
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
6.08 μM
Compound: 39
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
[PMID: 35964425]
HeLa IC50
4.78 μM
Compound: 39
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
[PMID: 35964425]
HepG2 IC50
3.48 μM
Compound: 39
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 35964425]
MCF7 IC50
1.83 μM
Compound: 39
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 35964425]
PC-3 IC50
12.74 μM
Compound: 39
Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
[PMID: 35964425]
WI-38 IC50
54.18 μM
Compound: 39
Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
[PMID: 35964425]
In Vitro

EGFR/HER2-IN-7 (compound 39) shows remarkable broad spectrum cytotoxic potency, with an IC50 value of 1.83 μM against MCF-7 breast cancer cell lines[1].
EGFR/HER2-IN-7 (1.83 μM) induces cell apoptosis by arreating cell cycle at G1/S[1].

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

EGFR/HER2/DHFR-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HepG2 hepatocellular carcinoma, MCF-7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate and Hea cervical epithelioid carcinoma
Concentration: 0-1 mM
Incubation Time: 72 hours
Result: Inhibited EGFR/HER2 kinase and DHFR, while DHFR inhibition caused cell cycle arrest at the S phase while EGFR/HER2 kinase inhibition caused arrest at the G1 phase.

Apoptosis Analysis[1]

Cell Line: HepG2 hepatocellular carcinoma, MCF-7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate and Hea cervical epithelioid carcinoma
Concentration: 0-1 mM
Incubation Time: 72 hours
Result: Inhibited cancer cells growth and induced apopsosis with IC50s of 3.48 μM (HepG2), 1.83 μM (MCF-7), 6.08 μM (HCT-116), 12.74 μM (PC3), 4.78 μM (Hela), respectively.
In Vivo

Caspase-3 is a lysosomal enzyme involved in apoptosis, and is used as a biomarker for detection of apoptotic cells[1].
EGFR/HER2-IN-7 (compound 39) (10 mg/kg; i.p.; once daily; 20 d) shows anti-breast cancer activity in vivo and increases caspase-3 immunoexpression in brease cancer mice[1].

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

Animal Model: Breast cancer with non-lactating mammary glands animal model in Swiss albino female mice (8-weeks-old)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; once daily; 20 days
Result: Inhibited tumor volume with reduction rate of 76.5%.
Reduced body weight with loss rate of 17.4%.
Showed the Caspase-3 score of 1.33.
Molecular Weight

379.23

Formula

C14H11BrN4O2S
CAS No.
SMILES

O=C(C1=CSC2=NC=C(C3=CC=C(Br)C=C3)N21)NNC(C)=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
References
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EGFR/HER2/DHFR-IN-1 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/HER2/DHFR-IN-12820126-37-0EGFREpidermal growth factor receptorErbB-1HER1thiazole Imidazo[2,1-b]thiazolein vivo?anti-breast cancer assaypharmacophore predictionInhibitorinhibitorinhibit

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