LY2157299

CAS No. 700874-72-2

LY2157299( Galunisertib | LY-2157299 | LY 2157299 )

Catalog No. M15689 CAS No. 700874-72-2

LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 36 In Stock
10MG 45 In Stock
50MG 111 In Stock
100MG 178 In Stock
200MG 268 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    LY2157299
  • Note
    Research use only, not for human use.
  • Brief Description
    LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM.
  • Description
    LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM; inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner, stimulates hematopoiesis from primary MDS bone marrow specimens; ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure; displays significant antitumor activity against both Calu6 and MX1 xenografts in mice.Blood Cancer Phase 3 Clinical(In Vitro):Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines.(In Vivo):Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration.
  • In Vitro
    Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines.
  • In Vivo
    Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration.
  • Synonyms
    Galunisertib | LY-2157299 | LY 2157299
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    TβRI
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    700874-72-2
  • Formula Weight
    369.4192
  • Molecular Formula
    C22H19N5O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 47 mg/mL
  • SMILES
    O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N
  • Chemical Name
    6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-

Shipping & Storage Information

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

Reference

1. Zhou L, et al. Cancer Res. 2011 Feb 1;71(3):955-63. 2. Yoon JH, et al. EMBO Mol Med. 2013 Nov;5(11):1720-39. 3. Bhola NE, et al. J Clin Invest. 2013 Mar;123(3):1348-58. 4. Rodon J, et al. Clin Cancer Res. 2015 Feb 1;21(3):553-60.
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