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CHMFL-PI3KD-317

Name: CHMFL-PI3KD-317
Brand: TargetMol
SKU: T10804
Price: 93 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T10804Cas No. 2244992-76-3

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting 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). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.

CHMFL-PI3KD-317

🥰Excellent

Purity: 99.16%

Catalog No. T10804Cas No. 2244992-76-3

Pack Size	Price	Availability
1 mg	$93	In Stock
5 mg	$228	In Stock
10 mg	$347	In Stock
25 mg	$625	In Stock
50 mg	$939	In Stock
100 mg	$1,280	In Stock
1 mL x 10 mM (in DMSO)	$248	In Stock

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Purity:99.16%

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COA LCMS

Product Introduction

Bioactivity

Description	CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting 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). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.
Targets&IC50	PI3Kγ:202.7 nM, PI3Kα:62.6 nM, PI4KIIIB:300.2 nM, PI3Kδ:6 nM, VPS34:1801.7 nM, PI4KIIIA:574.1 nM, PIK3C2B:882.3 nM, PI3Kβ:284 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 and, in Sprague-Dawley rats, shows favorable oral bioavailability and an acceptable half-life (T1/2 = 3.28 h).

Chemical Properties

Molecular Weight	494.03
Formula	C₂₁H₂₄ClN₅O₃S₂
Cas No.	2244992-76-3
Smiles	CC(C)[C@H](N)C(=O)Nc1nc(C)c(s1)-c1cnc(Cl)c(NS(=O)(=O)c2cccc(C)c2)c1
Relative Density.	1.406 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (91.09 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0242 mL	10.1208 mL	20.2417 mL	101.2084 mL
5 mM	0.4048 mL	2.0242 mL	4.0483 mL	20.2417 mL
10 mM	0.2024 mL	1.0121 mL	2.0242 mL	10.1208 mL
20 mM	0.1012 mL	0.5060 mL	1.0121 mL	5.0604 mL
50 mM	0.0405 mL	0.2024 mL	0.4048 mL	2.0242 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc