MNK1/2-IN-7
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970).
For research use only. We do not sell to patients.
- CAS No.: 2548283-27-6
- Formula: C31H31N5O2
- Molecular Weight:505.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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MNK1 4.4 nM (IC50, [1]) |
MNK2 0.4 nM (IC50, [1]) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.3 μM
Compound: 20j
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| DOHH-2 | IC50 |
0.9 μM
Compound: 20j
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Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| HT-29 | IC50 |
1.8 μM
Compound: 20j
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| LN-18 | IC50 |
0.91 μM
Compound: 20j
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Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| MDA-MB-231 | IC50 |
4.7 μM
Compound: 20j
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| PANC-1 | IC50 |
2.6 μM
Compound: 20j
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Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| PC-3 | IC50 |
25 μM
Compound: 20j
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Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
| TMD8 | IC50 |
4 μM
Compound: 20j
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Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
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[PMID: 38564512] |
MNK1/2-IN-7 (1.25-5 μM; 24 h) inhibits the phosphorylation of eIF4E in Hela cells (IC50=90.5 nM) and downregulates the phosphorylation of eIF4E and 4E-BP1 in A549 cells [1].
MNK1 /2-IN-7 shows stability in liver microparticles of humans, dogs, and rats, with T1/2 being 62.6 min, >120 min, and 64.6 min respectively[1].br /
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cell line
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Concentration:1.25 μM, 2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Downregulated the phosphorylation of eIF4E and 4E-BP1.
MNK1/2-IN-7 (10 mg/kg; po; 17 d) effectively caused tumor regression in a DOHH2 xenograft mouse model without affecting mouse body weight. MNK1/2-IN-7 also has a synergistic effect with Ibrutinib (HY-109970)[1].
Pharmacokinetic Analysis in SD Rats[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (μg/mL) | AUC0-t (h·μg/mL) | AUC0-∞ (h·μg/mL) | Cl (mL/h/kg) | F (%) |
| i.v. | 1 | 13.8 | 0.083 | 1.3 | 10.0 | 14.4 | 70.2 | / |
| p.o. | 5 | >24 | 6 | 1.5 | 23.3 | NA | / | 46.86 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GCB-DLBCL DOHH2 xenograft tumors model in mouse[1]
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Dosage:10 mg/kg
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Administration:po; once daily for 17 days; or combination of 3 mg/kg Ibrutinib
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Result:Resulted tumor regression
Achieved a greater TGI value of 54% for combination group at the end of treatment compared to the value for a single administration or ibrutinib administration.
Chemical Information
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CAS No. 2548283-27-6
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Molecular Weight 505.61
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Formula C31H31N5O2
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SMILES
O=C(C1=CC=C(C(C=C2)=NN3C2=NC=C3C4=CC5=C(O4)C=CC=C5)C=C1)N6CCC(CC6)N7CCCCC7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MNK1/2-IN-7 Related Classifications
HY-163479 Related Classifications
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