2. Cell Cycle/DNA Damage MAPK/ERK Pathway
  3. MNK Eukaryotic Initiation Factor (eIF)
  4. 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.

MNK1/2-IN-7

MNK1/2-IN-7 Chemical Structure

CAS No. : 2548283-27-6

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MNK1/2-IN-7 Related Antibodies

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Description

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)[1].

IC50 & Target

MNK1

4.4 nM (IC50, [1])

MNK2

0.4 nM (IC50, [1])

Cellular Effect
Cell Line Type Value Description References
A549 IC50
2.3 μM
Compound: 20j
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
[PMID: 38564512]
DOHH-2 IC50
0.9 μM
Compound: 20j
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
[PMID: 38564512]
HT-29 IC50
1.8 μM
Compound: 20j
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
[PMID: 38564512]
LN-18 IC50
0.91 μM
Compound: 20j
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
[PMID: 38564512]
MDA-MB-231 IC50
4.7 μM
Compound: 20j
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
[PMID: 38564512]
PANC-1 IC50
2.6 μM
Compound: 20j
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
[PMID: 38564512]
PC-3 IC50
25 μM
Compound: 20j
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
[PMID: 38564512]
TMD8 IC50
4 μM
Compound: 20j
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
[PMID: 38564512]
In Vitro

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.

MNK1/2-IN-7 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 cell line
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Downregulated the phosphorylation of eIF4E and 4E-BP1.
In Vivo

MNK1/2-IN-7 (5 mg/kg; po; single dose) exhibits acceptable exposure and bioavailability in rats and is orally effective [1].
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.

Animal Model: GCB-DLBCL DOHH2 xenograft tumors model in mouse[1]
Dosage: 10 mg/kg
Administration: po; once daily for 17 days; or combination of 3 mg/kg Ibrutinib
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.
Molecular Weight

505.61

Formula

C31H31N5O2
CAS No.
SMILES

O=C(C1=CC=C(C(C=C2)=NN3C2=NC=C3C4=CC5=C(O4)C=CC=C5)C=C1)N6CCC(CC6)N7CCCCC7
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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MNK1/2-IN-7 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:

MNK1/2-IN-72548283-27-6MNKEukaryotic Initiation Factor (eIF)Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseInhibitorinhibitorinhibit

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