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LY2157299

Chemical Structure : LY2157299

CAS No.: 700874-72-2

LY2157299 (Galunisertib;LY-2157299;LY 2157299)

Catalog No.: PC-43407Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI) with IC50 of 56 nM.
LY2157299 (Galunisertib) 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.
LY2157299 (Galunisertib) ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure.
LY2157299 (Galunisertib) displays significant antitumor activity against both Calu6 and MX1 xenografts in mice.

Physicochemical Properties

M.Wt 369.4192
Formula C22H19N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 47 mg/mL

Chemical Name/SMILES

6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-

References

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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