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IHMT-PI3K-455

Catalog No. T78836

IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ/δ dual inhibitor, demonstrating oral activity, with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ. This compound inhibits AKT phosphorylation and promotes tumor regression through the recruitment and activation of CD8+ T cells. It is utilized in cancer research [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

IHMT-PI3K-455, CAS N/A

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Biological Description

Chemical Properties

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Description	IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ/δ dual inhibitor, demonstrating oral activity, with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ. This compound inhibits AKT phosphorylation and promotes tumor regression through the recruitment and activation of CD8+ T cells. It is utilized in cancer research [1].
Targets&IC50	PI3Kα:6.717 μM, PI3Kβ:42.04 nM, PI3Kγ:7.1 nM, PI3Kδ:0.57 nM
In vitro	IHMT-PI3K-455 at a concentration of 1 μM for 2 hours inhibited AKT phosphorylation mediated by PI3Kγ/δ in RAW264.7 and Raji cells [1]. Additionally, when applied at the same concentration for 72 hours, it altered the polarization of M2 macrophages derived from THP-1 and BMDM cells [1].
In vivo	IHMT-PI3K-455 administered orally at a dose of 40 mg/kg once daily for 30 consecutive days inhibited tumor growth in the MC38 colorectal cancer murine allograft model [1]. This compound suppressed tumor proliferation by recruiting and activating an increased number of CD8+ cytotoxic T cells [1]. Additionally, pharmacokinetic parameters were assessed in Sprague-Dawley rats, revealing for a 1 mg/kg intravenous dose: Cmax (1233 ng/mL), Tmax (0.03 h), AUC0-∞ (477 h⋅ng/mL), T1/2 (1.59 h), CL (2.12 L/h/kg), Vz (4.80 L/kg); and for a 10 mg/kg oral dose: Cmax (157 ng/mL), Tmax (3.42 h), AUC0-∞ (838 h⋅ng/mL), T1/2 (2.71 h), CL (14.76 L/h/kg), Vz (56.02 L/kg), and F (17.6%).

Molecular Weight	517.49
Formula	C26H21F2N7O3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IHMT-PI3K-455 PI3K/Akt/mTOR signaling PI3K inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.