Cat. No.: HY-112608

CHMFL-PI3KD-317

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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.

For research use only. We do not sell to patients.

Purity: 98.04%
CAS No.: 2244992-76-3
Formula: C₂₁H₂₄ClN₅O₃S₂
Molecular Weight:494.03

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CHMFL-PI3KD-317 Chemical Structure

CAS No.: 2244992-76-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PI3Kδ

6 nM (IC₅₀)

PI3Kα

62.6 nM (IC₅₀)

PI3Kγ

202.7 nM (IC₅₀)

PI3Kβ

284 nM (IC₅₀)

PIK3C2B

882.3 nM (IC₅₀)

Vps34

1801.7 nM (IC₅₀)

PI4KIIIB

300.2 nM (IC₅₀)

PI4KIIIA

574.1 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	GI₅₀	3 μM Compound: 15i	Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-14	GI₅₀	3.3 μM Compound: 15i	Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MV4-11	GI₅₀	4.8 μM Compound: 15i	Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
NALM-6	GI₅₀	4 μM Compound: 15i	Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
PF-382	GI₅₀	3.5 μM Compound: 15i	Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T_1/2 = 3.28 h) in Sprague-Dawley rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nu/nu mice bearing MOLM-14 tumor xenografts^[1]
Dosage:

25, 50 and 100 mg/kg/day
Administration:

P.O. for 14 days
Result:

Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice.

Chemical Information

CAS No. 2244992-76-3
Appearance Solid
Molecular Weight 494.03
Formula C₂₁H₂₄ClN₅O₃S₂
Color White to off-white
SMILES

ClC1=C(NS(=O)(C2=CC(C)=CC=C2)=O)C=C(C3=C(C)N=C(NC([C@H](C(C)C)N)=O)S3)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (506.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0242 mL

10.1208 mL

20.2417 mL

5 mM

0.4048 mL

2.0242 mL

4.0483 mL

10 mM

0.2024 mL

1.0121 mL

2.0242 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0242 mL	10.1208 mL	20.2417 mL	50.6042 mL
	5 mM	0.4048 mL	2.0242 mL	4.0483 mL	10.1208 mL
	10 mM	0.2024 mL	1.0121 mL	2.0242 mL	5.0604 mL
	15 mM	0.1349 mL	0.6747 mL	1.3494 mL	3.3736 mL
	20 mM	0.1012 mL	0.5060 mL	1.0121 mL	2.5302 mL
	25 mM	0.0810 mL	0.4048 mL	0.8097 mL	2.0242 mL
	30 mM	0.0675 mL	0.3374 mL	0.6747 mL	1.6868 mL
	40 mM	0.0506 mL	0.2530 mL	0.5060 mL	1.2651 mL
	50 mM	0.0405 mL	0.2024 mL	0.4048 mL	1.0121 mL
	60 mM	0.0337 mL	0.1687 mL	0.3374 mL	0.8434 mL
	80 mM	0.0253 mL	0.1265 mL	0.2530 mL	0.6326 mL
	100 mM	0.0202 mL	0.1012 mL	0.2024 mL	0.5060 mL

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CHMFL-PI3KD-317

Kinase Inhibitor Library

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Multi-Target Compound Library

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Cell Proliferation Compound Library

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Posttranslational Modification Library

Lactylation Compound Library

All PI3K Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CHMFL-PI3KD-317 Related Classifications

HY-112608 Related Classifications