Products for Research Use Only

LY2157299

CAT: 0013-GTR19161710-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161710-01Size:500 mg
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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.
CAS Number
700874-72-2
Product Name Alternative
Galunisertib | LY-2157299 | LY 2157299
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
Molecular Formula
C22H19N5O
Molecular Weight
369.4192
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
6-Quinolinecarboxamide, 4-[5,6-dihydro-2- (6-methyl-2-pyridinyl) -4H-pyrrolo[1,2-b]pyrazol-3-yl]-

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