LY2157299

Specifications & Purity: ≥99%

For research use only. We do not sell to patients.

CAS#: 700874-72-2
Formula: C₂₂H₁₉N₅O
Molecular Weight : 369.42
PubChem CID: 10090485

Item Number

L126937

Grouped product items
SKU	Size	Availability	Price
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!	$189.90
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!	$251.90
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!	$722.90

Highly potent TGF-beta kinase antagonist

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Basic Description

Synonyms	LY-2157299;LY 2157299;Galunisertib;4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide;4-(2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
Specifications & Purity	≥99%
Storage Temp	Store at -20°C
Shipped In	Dry ice
Description	LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2/3. A potent TGF beta RI inhibitor.

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
PubChem CID	10090485
Molecular Weight	369.42

Database links

PubChem CID	10090485
ChEMBL Ligand	CHEMBL2364611
CAS Registry No.	700874-72-2

PubChem CID

10090485

ChEMBL Ligand

CHEMBL2364611

CAS Registry No.

700874-72-2

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

CTH Tchem Cystathionine gamma-lyase 7 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C7orf77 Tdark Uncharacterized protein C7orf77 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C8orf34 Tbio Uncharacterized protein C8orf34 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CGGBP1 Tbio CGG triplet repeat-binding protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C8orf76 Tdark Uncharacterized protein C8orf76 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHD1 Tbio Chromodomain-helicase-DNA-binding protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHERP Tbio Calcium homeostasis endoplasmic reticulum protein 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHP1 Tbio Calcineurin B homologous protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CAMTA2 Tbio Calmodulin-binding transcription activator 2 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNBD1 Tdark Cyclic nucleotide-binding domain-containing protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNBD2 Tdark Cyclic nucleotide-binding domain-containing protein 2 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

COMTD1 Tdark Catechol O-methyltransferase domain-containing protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NCAPD3 Tbio Condensin-2 complex subunit D3 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CMTR2 Tbio Cap-specific mRNA (nucleoside-2'-O-)-methyltransferase 2 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CTNNBIP1 Tbio Beta-catenin-interacting protein 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNDP2 Tbio Cytosolic non-specific dipeptidase 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE6H Tclin Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CTDNEP1 Tbio CTD nuclear envelope phosphatase 1 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNFN Tdark Cornifelin 0 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNKSR1 Tchem Connector enhancer of kinase suppressor of ras 1 30 Activities

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

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, 9 (6): (6659-6677). [PMID:29467918]