CHMFL-PI3KD-317

Modify Date: 2024-01-13 17:33:41

CHMFL-PI3KD-317 structure	Common Name	CHMFL-PI3KD-317
	CAS Number	2244992-76-3	Molecular Weight	494.03
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₂₄ClN₅O₃S₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of CHMFL-PI3KD-317

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50s 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[1].

Name	CHMFL-PI3KD-317
Synonym	More Synonyms

Description	CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50s 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[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Target	PI3Kδ:6 nM (IC50) PI3Kα:62.6 nM (IC50) PI3Kβ:284 nM (IC50) PI3Kγ:202.7 nM (IC50) PIK3C2B:882.3 nM (IC50) Vps34:1801.7 nM (IC50) PI4KIIIA:574.1 nM (IC50) PI4KIIIB:300.2 nM (IC50)
In Vitro	CHMFL-PI3KD-317 (Compound 15i) is a highly potent and selective PI3Kδ inhibitor, with an IC50s 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)[1]. In cellular assay, CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM[1]. CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.5 ± 0.8, 4.0 ± 0.9, 4.8 ± 0.2, 3.3 ± 0.2, 3.0 ± 0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively[1].
In Vivo	CHMFL-PI3KD-317 (Compound 15i) shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats[1]. CHMFL-PI3KD-317 (25, 50 and 100 mg/kg/day, p.o.) inhibits the growth of the MOLM14 tumor in mice[1].
References	[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.

Molecular Formula	C₂₁H₂₄ClN₅O₃S₂
Molecular Weight	494.03
Storage condition	-20°C

MFCD31813683

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: CHMFL-PI3KD-317
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: CHMFL-PI3KD-317
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: CHMFL-PI3KD-317
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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