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).

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MNK1/2-IN-7 Chemical Structure

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])

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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