OM-153 - ≥99% , CAS No.2406278-81-5

CAS: 2406278-81-5 Cat. No.: O646678 Molecular Weight: 509.53

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

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

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

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

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥99%

Names and Identifiers

• Molecular Weight: 509.53

Chemical and Physical Properties

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