AKR1C3-IN-17
AKR1C3-IN-17 is a cathepsin B (CTSB)-activated small molecule-drug conjugate targeting AKR1C3 with an IC50 of 9 nM. AKR1C3-IN-17 is cleaved by CTSB to release the payload Gemcitabine (HY-17026). AKR1C3-IN-17 induces apoptosis and shows antitumor activity in mice. AKR1C3-IN-17 can be used for the study of hepatocellular carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 3120497-79-9
- Formula: C38H43F2N7O11
- Molecular Weight:811.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
1.60 μM
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Inhibits the proliferation of HepG2 cells
Inhibits the proliferation of HepG2 cells
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42470376 |
AKR1C3-IN-17 (compound SM-27) (250 nM-1 μM; 24 h) induces cell cycle arrest at the S phase in HepG2 cells in a dose-dependent manner[1].
AKR1C3-IN-17 (250 nM-1 μM; 24 h) induces apoptosis in HepG2 cells in a dose-dependent manner, with total apoptotic rates of 1.34% (at 250 nM), 6.32% (at 500 nM) and 17.17% (at 1 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:250 nM, 500 nM, 1 μM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at S phase in a dose-dependent manner.
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Cell Line:HepG2
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Concentration:250 nM, 500 nM, 1 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner; total apoptotic rates were 1.34%, 6.32%, and 17.17%, respectively.
| Species | Dose | Route | T1/2 | CLz | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | Tmax | Vz | Cmax | Vz/F | CLz/F | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 3.45 h | 0.02 L/h/kg | 182.41 h·μg/L | 227.95 h·μg/L | 4.00 h | 5.28 h | 0.05 h | 0.06 L/kg | 47.60 μg/mL | / | / | / |
| Rat[1] | 5 mg/kg | i.g. | 4.27 h | / | 254.81 μg/L·h | 260.34 μg/L·h | 5.99 h | 6.72 h | 1.00 h | / | 33.65 μg/mL | 0.14 L/kg | 0.02 L/h/kg | 45.68 % |
AKR1C3-IN-17 (5 mg/kg; i.g.; q.d.; for 31 days) shows antitumor activity in the HepG2 mouse xenograft model, with a TGI of 60.24%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:2 mg/kg (i.v.); 5 mg/kg (i.g.)
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Administration:i.v. or i.g.; q.d. for 31 days
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Result:Showed significant antitumor activity with TGI of 76.27% (i.v., 2 mg/kg) and 60.24% (i.g., 5 mg/kg).
No significant body weight loss was observed in all treatment groups.
Revealed no significant damage to heart, liver, spleen, lung, and kidney.
Chemical Information
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CAS No. 3120497-79-9
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Molecular Weight 811.79
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Formula C38H43F2N7O11
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SMILES
COC1=CC(C(N[C@@H](C(C)C)C(N[C@H](C(NC2=NC(N(C=C2)[C@@H]3O[C@@H]([C@H](C3(F)F)O)CO)=O)=O)C)=O)=O)=CC(NC(C4=CC=CC=C4OCC5=C(ON=C5C)C)=O)=C1
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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)
AKR1C3-IN-17 Related Classifications
HY-187527 Related Classifications
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