1. Others Apoptosis Cell Cycle/DNA Damage
  2. Drug Derivative Apoptosis CDK ASK1
  3. MG16

MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer.

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MG16

MG16 Chemical Structure

CAS No. : 2349329-01-5

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Description

MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer[1].

IC50 & Target[1]

CDK6

 

In Vitro

MG16 (48 h) potently inhibits the proliferation of LLC, A549 and H446 lung cancer cells in vitro, with IC50 values of 408.2 ± 32.4, 613.1 ± 54.7 and 140.4 ± 10.4 nM[1], respectively.
Treatment with MG16 (0.1-100 nM; 48 h) induces dose-dependent apoptosis in A549 and H446 lung cancer cells, and its pro-apoptotic activity in both cell lines is significantly stronger than that of SN-38[1].
MG16 (90.1-1 μM for A549, 10-100 nM for H446; 24 h) regulates the expression of key apoptotic proteins and induces robust Caspase-3 activation in A549 and H446 lung cancer cells after 24 h of treatment, with a more prominent Caspase-3 activation effect than SN-38[1].
MG16 (613.1 nM; 48 h) induces cell cycle arrest at the G0/G1 phase in A549 lung cancer cells following 48 h of treatment at its IC50 concentration[1].

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

Western Blot Analysis[1]

Cell Line: A549 lung cancer cells, H446 lung cancer cells
Concentration: 0.1-1 μM (A549 cells); 10-100 nM (H446 cells)
Incubation Time: 24 h
Result: Upregulated the proapoptotic protein Bax, downregulated the antiapoptotic protein Bcl-2, and strongly activated caspase-3 in A549 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations.
Upregulated Bax, downregulated Bcl-2, and activated caspase-3 in H446 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations, especially at 100 nM.
In Vivo

MG16 (5 mg/kg; i.v.; every other day) achieves a 75.11% tumor inhibition rate, showing potent lung cancer growth suppression in a mouse LLC subcutaneous tumor model[1].
MG16 (5 mg/kg; i.v.; every other day) achieves an 80.5% tumor inhibition rate, showing potent lung cancer growth suppression in a mouse A549 subcutaneous tumor model[1].

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

Molecular Weight

471.89

Formula

C23H22ClN3O6

CAS No.
SMILES

CC[C@]1(C(OCC2=C1C=C3C4=NC5=CC=C(C=C5C=C4CN3C2=O)OC)=O)OC(CN)=O.Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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MG16
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HY-182071
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