PI3Kα-IN-9

CAS No. 2715287-67-3

PI3Kα-IN-9( —— )

Catalog No. M35579 CAS No. 2715287-67-3

PI3Kα-IN-9 is an orally available, selective and potent PI3Kα inhibitor with antiproliferative activity, inhibits PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, induces apoptosis, and can be used in the study of cancer.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 79 Get Quote
5MG 117 Get Quote
10MG 188 Get Quote
25MG 419 Get Quote
50MG 634 Get Quote
100MG 981 Get Quote
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Biological Information

  • Product Name
    PI3Kα-IN-9
  • Note
    Research use only, not for human use.
  • Brief Description
    PI3Kα-IN-9 is an orally available, selective and potent PI3Kα inhibitor with antiproliferative activity, inhibits PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, induces apoptosis, and can be used in the study of cancer.
  • Description
    PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research.
  • In Vitro
    PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis.PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K.Cell Viability Assay Cell Line:MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines Concentration:0-2 μM Incubation Time:72 hours Result:Inhibited the growth of a variety of cancer cells with IC50 values ranging from 0.43 to 1.33 μM.Apoptosis Analysis Cell Line:MGC-803 cells Concentration:0, 2, 4 and 8 μM Incubation Time:36 hours Result:Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.
  • In Vivo
    PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T1/2>10 h) and high bioavailability (130%).PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity.Animal Model:Male Sprague-Dawley ratDosage:1 and 10 mg/kg Administration:Oral administration and intravenous injection.Animal Model:Male BALB/c nude mice Dosage:30 mg/kg Administration:Oral administration; daily, for 3 weeks Result:Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis | PI3K
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2715287-67-3
  • Formula Weight
    383.4
  • Molecular Formula
    C18H21N7O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (260.82 mM; Ultrasonic (<80°C)
  • SMILES
    N1=C(N=C(N=C1N2CCOCC2)N3CCOCC3)C4=CC=C5OC(=NC5=C4)N
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Hou Y, et, al. Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. J Med Chem. 2022 Jul 14.?
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