CHMFL-PI3KD-317

CAS No. 2244992-76-3

CHMFL-PI3KD-317( —— )

Catalog No. M32845 CAS No. 2244992-76-3

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 236 In Stock
5MG 217 In Stock
10MG 330 In Stock
25MG 594 In Stock
50MG 873 In Stock
100MG 1190 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    CHMFL-PI3KD-317
  • Note
    Research use only, not for human use.
  • Brief Description
    CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM.
  • 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.
  • 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.
  • 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.CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2?=?3.28?h) in Sprague-Dawley rats.Animal Model:Female nu/nu mice bearing MOLM-14 tumor xenografts 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.
  • Synonyms
    ——
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    PI3K
  • Recptor
    PI3K | PI4K
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2244992-76-3
  • Formula Weight
    494.03
  • Molecular Formula
    C21H24ClN5O3S2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (506.04 mM; Ultrasonic )
  • SMILES
    CC(C)[C@H](N)C(=O)Nc1nc(C)c(s1)-c1cnc(Cl)c(NS(=O)(=O)c2cccc(C)c2)c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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?
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