OM-153 - ≥99% , CAS No.2406278-81-5

CAS: 2406278-81-5 Cat. No.: O646678 Formule: C₂₈H₂₄FN₇O₂ Poids moléculaire: 509.53

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Vue d’ensemble

OM-153 is a potent and orally active tankyrase inhibitor with IC 50 s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 ( TNKS1/2 ), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC 50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM

In Vitro

OM-153 shows picomolar IC 50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice. OM-153 decreases cell growth in COLO 320DM cells with a GI 50 value of 10 nM and a GI 25 value of 2.5 nM (concentrations resulting in 50% and 25% growth inhibition, respectively), while cell growth in RKO cells was insubstantially affected by the treatment. OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

OM-153 (0.1-10 mg/kg; p.o.; twice daily; for 34 days) reduces WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts. OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CB17-SCID mice bearing COLO 320DM cellsDosage: 10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg Administration: p.o.; twice daily; for 34 days Result: Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts. Animal Model: C57BL/6N mice injected with B16-F10 tumorsDosage: 10 mg/kg, 1 mg/kg, and 0.1 mg/kg Administration: p.o.; twice daily; for 20 days Result: Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect.

Form:Solid

IC50& Target:TNKS1|13 nM (IC|50|)|TNKS2|2 nM (IC|50|)|Wnt/β-catenin|0.63 nM (IC|50|)

Specifications

Spécifications et pureté

≥99%

Mécanismes biochimiques et physiologiques

OM-153 is a potent and orally active tankyrase inhibitor with IC 50 s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 ( TNKS1/2 ), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC 50 value of 0.63 nM. O

Conditions de stockage de stockage

Store at -20°C

Expédié en

Ice chest + Ice pads

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: 509.53

Propriétés chimiques et physiques

• Solubilité: DMSO : 100 mg/mL (196.26 mM; Need ultrasonic)

Foire aux questions

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2406278-81-5, the molecular formula is C28H24FN7O2, and the molecular weight is 509.53 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.