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LY2109761

(CAS: 700874-71-1)

Suppliers of LY2109761

Company Name Email Tel Country
Active Biopharma Corp [email protected] +86 (571) 8161-2335 China

Fax: Purity: Brand:

Apexbio Technology LLC [email protected] +1-832-696-8203 USA

Fax: +1-832-641-3177Purity: 98% Brand: Tocris

BOC Sciences [email protected] 1-631-504-6093

Fax: 1-631-614-7828Purity: Brand: BOC Sciences

Biochempartner Co., Ltd [email protected] 0086-13720134139; 0086-15971444841 China

Fax: Purity: 98% Brand: Biochempartner

CHEMSCENE, LLC [email protected] 732-484-9848 USA

Fax: 888-484-5008Purity: Brand:

Price and Availability: USD108/5mg () USD180/10mg ()

MedChemexpress Co., Ltd. [email protected] 609-228-6898 USA

Fax: 609-228-5909Purity: Brand:

Price and Availability: USD108/5mg () USD180/10mg ()
Quality Control & MSDS Files: HNMR HNMR LCMS LCMS MSDS

Selleck Chemicals LLC [email protected] +1-832-582-8158 USA

Fax: +1-832-582-8590Purity: >98% Brand:

Price and Availability: USD270/5mg (In stock) USD370/10mg (In stock) USD432/10mM/1mLIn DMSO (In stock) USD1070/50mg (In stock) USD2470/200mg (In stock)
Quality Control & MSDS Files: HPLC

Shanghai Haoyuan Chemexpress Co., Ltd. [email protected] +86 (21) 5187-0955 / +86 (21) 5895-5995 China

Fax: +86 (21) 5895-5996Purity: Brand:

Price and Availability: USD108/5mg () USD180/10mg ()

Target Molecule Corp. [email protected] (857) 239-0968 USA

Fax: 857-239-8801Purity: .98 Brand: TargetMol

Price and Availability: USD174/10mg () USD348/25mg () USD648/50mg ()

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Background Information of LY2109761

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2. IC50 value: 38 nM/300 nM(Ki, TβRI/II) [1] Target: TGF-β receptor type I/II in vitro: LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581.

Solubility of LY2109761

Solubility Sources
Limited solubility Apexbio Technology LLC
DMSO MedChemexpress Co., Ltd.
DMSO <1 mg/mL (<1 mM) ; Water <1 mg/mL (<1 mM) ; Ethanol <1 mg/mL (<1 mM) Selleck Chemicals LLC

Storage Condition of LY2109761

Storage Condition Sources
Store at -20°C Apexbio Technology LLC

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[HNMR] [LCMS] MedChemexpress Co., Ltd.
[HPLC] Selleck Chemicals LLC

Mechanism and Indications

Signaling Pathways TGF-beta/Smad Autophagy
Target Autophagy TGF-β Receptor
Research Area Cancer
Indications Glioblastoma Hepatocellular carcinoma Glioma

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LY2109761 Eli Lilly & Co Glioblastoma 2012/4/30 2014/8/31 Phase 2 Clinical
LY2109761 Eli Lilly & Co Hepatocellular carcinoma 2011/3/31 2015/5/31 Phase 2 Clinical
LY2109761 Eli Lilly & Co Glioma 2011/4/30 2015/1/31 Phase 2 Clinical
LY2109761 Eli Lilly & Co 2013/10/31 2013/11/30 Phase 1 Clinical
LY2109761 Eli Lilly & Co 2013/1/31 2013/2/28 Phase 1 Clinical
LY2109761 - No Development Reported

Chemical Information

M.Wt Formula CAS No. Synonyms
441.52 C26H27N5O2 700874-71-1 LY 2109761;LY-2109761; 4-(2-((4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl)oxy)ethyl)morpholine

Structure Information of LY2109761

Smiles N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6
InChI InChI=1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2

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Chemical and Physical Properties

Appearance:White to off-white solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:

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