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LY2157299

CAT: 0013-GTR19161710-05Size: 50 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161710-05Size:50 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]-

Chemical Information

Galunisertib

LY-2157299 is a pyrrolopyrazole that is 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole which is substituted at positions 2 and 3 by 6-methylpyridin-2-yl and 6-(aminocarbonyl)quinolin-4-yl groups, respectively. A Transforming growth factor-betaRI (TGF-betaRI) kinase inhibitor, it blocks TGF-beta-mediated tumor growth in glioblastoma. It has a role as an antineoplastic agent and a TGFbeta receptor antagonist. It is a member of methylpyridines, a member of quinolines, a monocarboxylic acid amide, a pyrrolopyrazole and an aromatic amide.

CAS Number700874-72-2
PubChem CID10090485
IUPAC Name4-[2-(6-methyl-2-pyridinyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide
Molecular FormulaC22H19N5O
Molecular Weight369.4
XLogP2.4
Topological Polar Surface Area86.7
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Heavy Atom Count28
Formal Charge0
Complexity585
SMILES
CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N
InChI
InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
InChIKey
IVRXNBXKWIJUQB-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Galunisertib
CAS: 700874-72-2
CID: 10090485
Formula: C22H19N5O
MW: 369.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight369.4
XLogP32.4
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Exact Mass369.15896025
Monoisotopic Mass369.15896025
Topological Polar Surface Area86.7 Ų
Heavy Atom Count28
Formal Charge0
Complexity585
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
MBS3605687-01LY2157299
C16713-10mgGalunisertib (LY2157299)

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