IHMT-PI3Kδ-372 free base · Synonyms: IHMT-PI3Kδ-372 S-isomer | IHMT-PI3Kdelta-372

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K Cytochrome P450

Research area Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

IHMT-PI3Kδ-372 structure

CAS No.: 2429889-61-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 420.00	BP-02015-25mg	In stock	Get quote
50 mg	USD 620.00	BP-02015-50mg	In stock	Get quote
100 mg	USD 880.00	BP-02015-100mg	In stock	Get quote
250 mg	USD 1,480.00	BP-02015-250mg	In stock	Get quote
500 mg	Inquire	BP-02015-500mg	Inquire	Inquire
1 g	Inquire	BP-02015-1g	Inquire	Inquire

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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.

Biological activity

In Vitro IHMT-PI3Kδ-372 (Compound (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 (compound (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). In Vivo IHMT-PI3Kδ-372 (Compound (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 decreases the inflammatory cell infiltration in a dose-dependent manner. In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (compound (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 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes.

Identifiers

SMILES: CC[C@@H](C(N1C2CC2)=NC3=CC=CC(F)=C3C1=O)N4C5=NC=NC(N)=C5C(C6=CC(F)=C(C=C6)OC)=N4
InChIKey: HTUBTEAYSCSTIY-SFHVURJKSA-N

Specifications

MW (average): 503.5033
Formula: C₂₆H₂₃F₂N₇O₂
CAS No.: 2429889-61-0
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 50 mg/mL

Documents

References

[1]. Li F, Liang X, Jiang Z, 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;63(22):13973-13993. doi:10.1021/acs.jmedchem.0c01544

Same target

Search PI3K

Same research area

Search Inflammation/Immunology