DS89002333 - ≥99% , CAS No.2832159-79-0

CAS: 2832159-79-0 Cat. No.: D649090 Formule: C₂₂H₂₀ClF₂N₃O₃ Poids moléculaire: 447.86

GRADE & PURITY ≥99%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

Vue d’ensemble

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC 50 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)

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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 IC 50 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 . DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model . 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) . 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) . 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.

Form:Solid

IC50& Target:PRKACA 0.3 nM (IC 50 )

Specifications

Spécifications et pureté

≥99%

Mécanismes biochimiques et physiologiques

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC 50 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 fibr

Conditions de stockage de stockage

Store at 2-8°C,Protected from light,Desiccated

Expédié en

Wet ice

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Pureté

≥99%

Noms et identifiants

• Poids moléculaire: 447.86

Propriétés chimiques et physiques

• Solubilité: DMSO : 100 mg/mL (223.28 mM; Need ultrasonic)