1. PI3K/Akt/mTOR
  2. PI3K
  3. CHMFL-PI3KD-317

CHMFL-PI3KD-317 

Cat. No.: HY-112608
Handling Instructions

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.

CHMFL-PI3KD-317 Chemical Structure

CHMFL-PI3KD-317 Chemical Structure

CAS No. : 2244992-76-3

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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[1].

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)

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].

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 (T1/2 = 3.28 h) in Sprague-Dawley rats[1].

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.
Molecular Weight

494.03

Formula

C₂₁H₂₄ClN₅O₃S₂

CAS No.

2244992-76-3

SMILES

ClC1=C(NS(=O)(C2=CC(C)=CC=C2)=O)C=C(C3=C(C)N=C(NC([[email protected]](C(C)C)N)=O)S3)C=N1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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CHMFL-PI3KD-317
Cat. No.:
HY-112608
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