CHMFL-PI3KD-317

• UNSPSC 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].

• Target Antigen:

  PI3K

• Type:

  Reference compound

• Related Pathways:

  PI3K/Akt/mTOR

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/CHMFL-PI3KD-317.html

• Purity:

  98.04

• Solubility:

  DMSO : 250 mg/mL (ultrasonic)

• 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

• Molecular Weight:

  494.03

• References & Citations:

  [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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  2244992-76-3