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IHMT-PI3Kδ-372 S-isomer

Catalog No. T60196 CAS 2429889-61-0

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

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IHMT-PI3Kδ-372 S-isomer Chemical Structure

IHMT-PI3Kδ-372 S-isomer, CAS 2429889-61-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
2 mg	In stock	$ 293.00
5 mg	In stock	$ 448.00
10 mg	In stock	$ 658.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,380.00
100 mg	In stock	$ 1,890.00
1 mL * 10 mM (in DMSO)	In stock	$ 545.00

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Purity: 99.68%

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Description	IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
In vitro	IHMT-PI3Kδ-372 (S)-18 (0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC50 value of 67 nM. IHMT-PI3Kδ-372 (S)-18 shows moderate inhibition of CYP2C9 (IC50 of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC50s > 10 μM)[1].
In vivo	IHMT-PI3Kδ-372 (S)-18; 1-5 mg/kg; inhalation; daily; for 28 days) improves lung function and reduced the inflammatory patterns characteristic of COPD. The lung function parameters such as forced expiratory volume in the first second (FEV1), forced vital capacity (FVC), and peak expiratory flow (PEF) are improved dose-dependently. The abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes are also reduced. IHMT-PI3Kδ-372 (S)-18 decreases the inflammatory cell infiltration in a dose-dependent manner. In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (S)-18 displays a half-life of 2.3 h, low exposure of 66 ng/mL, and high clearance of 348.5 mL/min/kg in plasma but high exposure of 5599 ng/g (6 h after inhalation) in lung tissue. IHMT-PI3Kδ-372 (S)-18 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes[1].

Molecular Weight	503.5
Formula	C26H23F2N7O2
CAS No.	2429889-61-0

Storage

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

Solubility Information

DMSO: 50 mg/mL (99.3 mM)

References and Literature

1. Li F, et al. Discovery of (S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease. J Med Chem. 2020 Nov 25;63(22):13973-13993.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Obesity Compound Library Anti-Breast Cancer Compound Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Antioxidant Compound Library Antidepressant Compound Library

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Keywords

IHMT-PI3Kδ-372 S-isomer 2429889-61-0 PI3K/Akt/mTOR signaling PI3K IHMTPI3Kδ372Sisomer IHMT-PI3Kdelta-372 S-isomer inhibitor inhibit

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