[CAS NO. 700874-72-2] Galunisertib (LY2157299)

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PRODUCTS SPECIFICATIONS [700874-72-2]

Catalog

SLK-S2230

Brand

Selleck

CAS

700874-72-2

DESCRIPTION [700874-72-2]

Overview

MDL	MFCD12923319
Molecular Weight	369.42
Molecular Formula	C22H19N5O
SMILES	CC1=NC(C=2C(=C3N(N2)CCC3)C=4C5=C(C=CC(C(N)=O)=C5)N=CC4)=CC=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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
50 mM	0.0541 mL	0.2707 mL	0.5414 mL

Description

Galunisertib (LY2157299) is a potent inhibitor with of 56 nM in a cell-free assay. Phase 2/3.

Targets

TβRI ^[1]
(Cell-free assay)

56 nM

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. 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. In human glioblastoma (GBM) cells, LY2157299 treatment blocks signaling through the heteromeric TGFβ receptor complex to reduce levels of active, phosphorylated SMAD.

References

[1] Mundla SR, Patent, 2006, US7872020.
[2] Yingling JM, et al. Proc Am Assoc Cancer Res. 2006, 47, abstract 250.
[3] Zhou L, et al. Cancer Res, 2011, 71(3), 955-963.
[4] Parsons S, et al. Mol Cancer Ther, 2011, 10(11), Suppl 1, Abst C201.
[5] Bueno L, et al. Eur J Cancer, 2008, 44(1), 142-150.
[6] Liu Z, et al. J Cell Sci, 2009, 122(18), 3294-3302.
[7] Peng S, et al. Int J Biol Sci. 2022 Feb 21;18(5):1912-1932.

Synonyms

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

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

LY 2157299

Galunisertib