
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)






Size | Price / USD | Stock | Quantity |
5MG | 36 | In Stock |
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10MG | 45 | In Stock |
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50MG | 111 | In Stock |
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100MG | 178 | In Stock |
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200MG | 268 | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameLY2157299
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NoteResearch use only, not for human use.
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Brief DescriptionLY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM.
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DescriptionLY2157299 (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.
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In VitroGalunisertib (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.
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In VivoHuman 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.
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SynonymsGalunisertib | LY-2157299 | LY 2157299
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PathwayTGF-beta/Smad
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TargetTGFBR
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RecptorTβRI
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number700874-72-2
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Formula Weight369.4192
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Molecular FormulaC22H19N5O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 47 mg/mL
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SMILESO=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N
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Chemical Name6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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.
molnova catalog



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