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Signaling Pathway

LY2157299

HY-13226

(Galunisertib; LY-2157299; LY 2157299)

LY2157299

LY2157299 Chemical Structure

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $109 In-stock
5 mg $99 In-stock
10 mg $135 In-stock
50 mg $405 In-stock
100 mg $750 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €107 In-stock
5 mg €97 In-stock
10 mg €132 In-stock
50 mg €397 In-stock
100 mg €735 In-stock
200 mg Get quote
500 mg Get quote

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Inquiry Information
Product name: LY2157299
Cat. No.: HY-13226

LY2157299 Data Sheet

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    Purity: 99.88%

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Biological Activity of LY2157299

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.
IC50 value: 56 nM [1]
Target: TGFβ receptor I
in vitro: LY2157299 potently inhibits the TGFβ receptor signaling. LY2157299 abolishes the TGFβ induced Smad2 phosphorylation in HUVEC cells. LY2157299 also shows dose dependent potentiation of VEGF or bFGF induced cell proliferation in HUVEC. LY2157299 also promotes VEGF induced HUVEC cell migration. LY2157299 potentiates angiogenesis in the in vitro VEGF-stimulated cord formation assay [2]. LY2157299 inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner. LY2157199 treatment stimulates hematopoiesis from primary MDS bone marrow specimens [3].
in vivo: Although anti-tumor activity has been observed in several pre-clinical models, LY2157299 fails to show significant in vivo angiogenic effects in the 4T1, Colo205, or A549 xenograft models [2]. Administration of LY2157299 ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. [3] Oral administration of LY2157299 at 75 mg/kg/day displays significant antitumor activity against both Calu6 and MX1 xenografts in mice [3].

Chemical Information

M.Wt 369.42 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C22H19N5O
CAS No 700874-72-2
Solvent & Solubility

DMSO:52mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.7069 mL 13.5347 mL 27.0695 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL

Clinical Information of LY2157299

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
LY2157299 Eli Lilly & Co 31-OCT-13 30-NOV-13 Phase 1 25-NOV-13
Eli Lilly & Co Advanced solid tumor 30-NOV-12 30-APR-14 Phase 1 20-NOV-13
Eli Lilly & Co 31-JAN-13 28-FEB-13 Phase 1 18-FEB-13
Eli Lilly & Co Glioma 30-APR-11 31-JAN-15 Phase 2 11-NOV-13
Eli Lilly & Co Hepatocellular carcinoma 31-MAR-11 31-MAY-15 Phase 2 15-NOV-13

References on LY2157299

Inhibitor Kit

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