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CHMFL-PI3KD-317

Catalog No. T10804 CAS 2244992-76-3

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.

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CHMFL-PI3KD-317, CAS 2244992-76-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 112.00
5 mg	In stock	$ 278.00
10 mg	In stock	$ 447.00
25 mg	In stock	$ 739.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,390.00
500 mg	In stock	$ 2,820.00
1 mL * 10 mM (in DMSO)	In stock	$ 297.00

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Purity: 97.8%

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Storage & Solubility Information

Description	CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
Targets&IC50	PI3Kδ:6 nM, Vps34:1801.7 nM, PI3Kβ:284 nM, PIK3C2B:882.3 nM, PI4KIIIA:574.1 nM, PI3Kα:62.6 nM, PI3Kγ:202.7 nM, PI4KIIIB:300.2 nM
In vitro	CHMFL-PI3KD-317 exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 4.0, 3.5, 4.8, 3.0, 3.3 μM against NALM-6, PF382, MV4-11, MOLM-13 cells, and MOLM-14, respectively.
In vivo	CHMFL-PI3KD-317 (Compound 15i; 25, 50, and 100 mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice. In Sprague-Dawley rats, CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h).

Molecular Weight	494.03
Formula	C21H24ClN5O3S2
CAS No.	2244992-76-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 45 mg/mL (91.09 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Liang X, et al. Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. Eur J Med Chem. 2018 Aug 5;156:831-846.

Related compound libraries

This product is contained In the following compound libraries：

Metabolism Compound Library Anti-Obesity Compound Library Anti-Breast Cancer Compound Library Neuronal Differentiation Compound Library Anti-Ovarian Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compound Library Antidepressant Compound Library Inhibitor Library

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Related compounds with same targets

Sennidin A Sennidin B AZD3458 PI3kδ inhibitor 1 Isoangustone A PI3K/mTOR Inhibitor-1 PI3Kdelta inhibitor 1 α-Solanine

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Keywords

CHMFL-PI3KD-317 2244992-76-3 PI3K/Akt/mTOR signaling PI3K PI4K CHMFL-PI-3KD-317 CHMFLPI3KD317 CHMFL PI3KD 317 inhibitor inhibit

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