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  3. DS89002333

DS89002333 

Cat. No.: HY-150072
Handling Instructions

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC).

For research use only. We do not sell to patients.

DS89002333 Chemical Structure

DS89002333 Chemical Structure

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Description

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC)[1].

IC50 & Target

PRKACA

0.3 nM (IC50)

In Vitro

DS89002333 (0.001, 0.01, 0.1, 1, 10 µM; 30 min) inhibits phosphorylation of CREB in a dose-dependent manner in NIH/3T3 cells (phosphorylation status of CREB as a marker of intracellular PRAKACA inhibitory activity)[1].

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

Cell Viability Assay[1]

Cell Line: NIH/3T3 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 µM
Incubation Time: 30 min
Result: Showed a dose-dependent decrease in phosphorylation of CREB, with an IC50 of 50 nM.
In Vivo

DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model[1].
DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model[1].

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

Animal Model: Female nude mice (NIH/3T3-fusion allograft model)[1].
Dosage: 12.5, 50 mg/kg
Administration: Oral administration, twice daliy for 5 days.
Result: Exhibited anti-tumor activity without body weight loss.
Animal Model: Female NOD SCID mice (FL-HCC PDX xenograft model)[1].
Dosage: 3, 30 mg/kg
Administration: Oral administration, twice daliy for 22 days.
Result: Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.
Molecular Weight

447.86

Formula

C22H20ClF2N3O3

SMILES

O=C(NC([[email protected]]1([H])C[[email protected]@H](O)CN1)C2=CC(Cl)=C(F)C=C2)C3=CC4=CC=NC(F)=C4C=C3OC

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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DS89002333
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HY-150072
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