2. Metabolic Enzyme/Protease JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. Dihydrofolate reductase (DHFR) EGFR
  4. DHFR-IN-4

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.

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

DHFR-IN-4 Chemical Structure

DHFR-IN-4 Chemical Structure

CAS No. : 2820126-49-4

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Based on 1 publication(s) in Google Scholar

DHFR-IN-4 Related Antibodies

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

  • Biological Activity

  • Purity & Documentation

  • References

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Description

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells[1].

IC50 & Target

IC50: 123 nM (DHFR), 246 nM (EGFR), 357 nM (HER2)[1]
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
13.24 μM
Compound: 42
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
6.9 μM
Compound: 42
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
9.67 μM
Compound: 42
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
8.46 μM
Compound: 42
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
11.17 μM
Compound: 42
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
89.61 μM
Compound: 42
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

DHFR-IN-4 (compound 42) (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency against HepG2, MCF-7, HCT-116, PC3 and HeLa[1].

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

DHFR-IN-4 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, MCF-7, HCT-116, PC3 and HeLa
Concentration: 0-100 μM
Incubation Time: 72 h
Result: Exhibited antiproliferative activity against HepG2, MCF-7, HCT-116, PC3 and HeLa with IC50s of 9.67±0.7 μM, 8.46±0.7 μM, 13.24±0.9 μM, 11.17±1.0 μM and 6.90±0.5 μM.
Molecular Weight

371.46

Formula

C18H21N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CSC2=NC(CN3CCOCC3)=C(C4=CC=C(C)C=C4)N21)NN
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 (336.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6921 mL 13.4604 mL 26.9208 mL
5 mM 0.5384 mL 2.6921 mL 5.3842 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6921 mL 13.4604 mL 26.9208 mL 67.3020 mL
5 mM 0.5384 mL 2.6921 mL 5.3842 mL 13.4604 mL
10 mM 0.2692 mL 1.3460 mL 2.6921 mL 6.7302 mL
15 mM 0.1795 mL 0.8974 mL 1.7947 mL 4.4868 mL
20 mM 0.1346 mL 0.6730 mL 1.3460 mL 3.3651 mL
25 mM 0.1077 mL 0.5384 mL 1.0768 mL 2.6921 mL
30 mM 0.0897 mL 0.4487 mL 0.8974 mL 2.2434 mL
40 mM 0.0673 mL 0.3365 mL 0.6730 mL 1.6825 mL
50 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.3460 mL
60 mM 0.0449 mL 0.2243 mL 0.4487 mL 1.1217 mL
80 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6730 mL
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DHFR-IN-4 Related Classifications

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:

DHFR-IN-42820126-49-4Dihydrofolate reductase (DHFR)EGFREpidermal growth factor receptorErbB-1HER1dihydrofolate reductaseDHFRanticancerHepG2MCF-7HCT-116PC3HeLaInhibitorinhibitorinhibit

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