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LY2157299 - ≥99%, high purity , TGF-beta receptor type I inhibitor, CAS No.700874-72-2, TGF-beta receptor type I inhibitor

Specifications & Purity:  ≥99%
Item Number
L126937
Grouped product items
SKUSizeAvailabilityPrice Qty
L126937-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$48.90
L126937-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$68.90
L126937-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$147.90

Highly potent TGF-beta kinase antagonist

Basic Description

SynonymsGalunisertib|700874-72-2|LY2157299|LY 2157299|LY-2157299|4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide|ly2157299(galunisertib)|UNII-3OKH1W5LZE|Galunisertib (LY2157299)|Galunisertib [USAN]|3OKH1W5LZE|4-[2-(6-
Specifications & Purity≥99%
Storage TempStore at -20°C
Shipped InDry ice
Action TypeINHIBITOR
Mechanism of actionTGF-beta receptor type I inhibitor

Product Properties

ALogP2.4

Associated Targets

TGFBR1 Tchem TGF-beta receptor type-1 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TGFBR2 Tchem TGF-beta receptor type-2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RIPK3 Tchem Receptor-interacting serine/threonine-protein kinase 3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MINK1 Tchem Misshapen-like kinase 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BMPR1B Tchem Bone morphogenetic protein receptor type-1B 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ACVR1B Tchem Activin receptor type-1B 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide
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)
InChi Key IVRXNBXKWIJUQB-UHFFFAOYSA-N
Canonical SMILES CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N
Isomeric SMILES CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N
PubChem CID 10090485
Molecular Weight 369.42

Certificates

Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
J1521097Certificate of AnalysisMay 10, 2023 L126937

Chemical and Physical Properties

SolubilityDMSO 74 mg/mL (200.31 mM); Water <1 mg/mL (<1 mM);Ethanol <1 mg/mL (<1 mM)

Related Documents

References

1. Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD et al..  (2008)  Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent..  J Med Chem,  51  (7): (2302-6).  [PMID:18314943]
2. Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW et al..  (2018)  Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor..  Oncotarget,  (6): (6659-6677).  [PMID:29467918]

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