IHMT-PI3K-455
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8+ killing T cells.IHMT-PI3K-455 is used in cancer research.
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- CAS No.: 3047746-40-4
- Formule: C26H21F2N7O3
- Masse moléculaire:517.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PI3Kα 6.717 μM (IC50) |
PI3Kβ 42.04 nM (IC50) |
PI3Kγ 7.1 nM (IC50) |
PI3Kδ 0.57 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | GI50 |
>10 μM
Compound: 15u
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Growth inhibition of CHO cells measured after 72 hrs by celltiter-glo assay
Growth inhibition of CHO cells measured after 72 hrs by celltiter-glo assay
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[PMID: 37683362] |
| MCF-10A | GI50 |
>10 μM
Compound: 15u
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Growth inhibition of human MCF-10A cells measured after 72 hrs by celltiter-glo assay
Growth inhibition of human MCF-10A cells measured after 72 hrs by celltiter-glo assay
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[PMID: 37683362] |
IHMT-PI3K-455 (1 μM, 2 h) suppresses the PI3Kγ/δ-mediated AKT phosphorylation in RAW264.7 cells and Raji cells[1].
IHMT-PI3K-455 (1 μM, 72 h) alters the macrophage polarization in M2 macrophages derived from THP-1 and BMDM cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Macrophages
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Concentration:0.1, 1 μM
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Incubation Time:72 h
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Result:Increased the proinflammatory M1 macrophage phenotype in a dose-dependent manner, with a concomitant dose-dependent decrease of the anti-inflammatory M2 macrophage phenotype.
Repolarized M2 phenotype toward M1 phenotype in THP-1 and BMDM macrophages.
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Cell Line:RAW264.7 cells; Raji cells
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Concentration:0, 0.01, 0.03, 0.1, 0.3, 1 μM
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Incubation Time:2 h
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Result:Potently inhibited the PI3Kγ-mediated AKT473 phosphorylation in RAW264.7 cells (human C5a stimulation) with an IC50 value of 0.015 μM.
Potently inhibited the PI3Kδ-mediated AKT473 phosphorylation in Raji cells (anti-IgM stimulation) with an IC50 value of 0.010 μM.
IHMT-PI3K-455 (40 mg/kg for p.o; once daily for 30 days) inhibits tumor growth by recruiting and activating more CD8+ killing T cells[1].
Pharmacokinetic parameters of IHMT-PI3K-455 in Sprague-Dawley rats[1]
| Dose (mg/kg) | Administration route | Cmax (ng/mL) | Tmax (h) | AUC0-∞ (h?ng/mL) | T1/2 (h) | CL (L/h/kg) | Vz (L/kg) | F (%) |
| 1 | i.v. | 1233 | 0.03 | 477 | 1.59 | 2.12 | 4.80 | - |
| 10 | p.o. | 157 | 3.42 | 838 | 2.71 | 14.76 | 56.02 | 17.6 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MC38 tumor model[1]
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Dosage:10 mg/kg, 40 mg/kg
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Administration:Oral gavage (p.o.); Once daily for 30 days
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Result:Significantly inhibited tumor size in a dose-dependent manner.
Increased tumor-infiltrating CD8+T cells.
Chemical Information
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CAS No. 3047746-40-4
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Masse moléculaire 517.49
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Formule C26H21F2N7O3
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SMILES
COC1=C(OC)N=CC(C2=NC3=CC(NC4=CC=CC(CNC(C5=C(F)C=CC=C5F)=O)=N4)=NN3C=C2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IHMT-PI3K-455 Related Classifications
HY-149493 Related Classifications
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