LY2940680

Modify Date: 2025-08-25 19:10:11

LY2940680 structure	Common Name	LY2940680
	CAS Number	1258861-20-9	Molecular Weight	512.502
	Density	1.4±0.1 g/cm3	Boiling Point	703.5±60.0 °C at 760 mmHg
	Molecular Formula	C₂₆H₂₄F₄N₆O	Melting Point	N/A
	MSDS	N/A	Flash Point	379.3±32.9 °C

Use of LY2940680

Taladegib (LY2940680) is an antagonist of the smoothened receptor.

Name	4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
Synonym	More Synonyms

Description	Taladegib (LY2940680) is an antagonist of the smoothened receptor.
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> Smo Research Areas >> Cancer
Target	Smo[1]
In Vitro	Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC50: Taladegib=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC50: Taladegib=61.2±21.1 μM)[1]. The IC50 for Taladegib inhibition of [3H]MRT-92 binding is right shifted (3- to 100-fold) for the S387AECL2, L325F3.36f, and D473H6.54f mutants but did not differ from that of WT receptor for the other mutants. The ability of SANT-1 to inhibit [3H]MRT-92 binding to V329F3.40f and T466F6.47f mutants is abolished, and it is severely impaired for L325F3.40f, I408F5.51f, and M525G7.45f mutants (4- to 140-fold drop of the IC50), but is not modified for the S387AECL2 mutant. Taken together, these data confirm our docking hypothesis that MRT-92-binding mode differs from that of either Taladegib or SANT-1 by simultaneously occupying binding sites 1 and 2[2].
References	[1]. Fraveto A, et al, Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures. PLoS One. 2015 Nov 16;10(11):e0142124. [2]. Hoch L, et al. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J. 2015 May;29(5):1817-29. [3]. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246.

Density	1.4±0.1 g/cm3
Boiling Point	703.5±60.0 °C at 760 mmHg
Molecular Formula	C₂₆H₂₄F₄N₆O
Molecular Weight	512.502
Flash Point	379.3±32.9 °C
Exact Mass	512.194763
PSA	67.15000
LogP	2.70
Vapour Pressure	0.0±2.2 mmHg at 25°C
Index of Refraction	1.634
Storage condition	-20°C

Hazard Codes	Xi

N-methyl-1-[4-(...

CAS#:1258861-50-5

4-Fluoro-2-(tri...

CAS#:189807-21-4

~83%

LY2940680

CAS#:1258861-20-9

Literature: US2010/324048 A1, ; Page/Page column 6 ;

Precursor 1
CAS#:189807-21-4 4-Fluoro-2-(tri...
DownStream 0

Name: Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
Source: NCGC
Target: N/A
External Id: SERCaMPGLuc-p1-antagonist

Name: Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (...
Source: NCGC
External Id: IP6K1-p1

Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase

Name: Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ...
Source: NCGC
External Id: huntington-HTTAS8-p1-FF-overN

Name: Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu...
Source: NCGC
External Id: CYP3A4437

Name: Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu...
Source: NCGC
External Id: CYP2D6395

Name: Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu...
Source: NCGC
External Id: CYP2C9536

Name: Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
Source: NCGC
Target: N/A
External Id: TRND-SARS-CoV-2-cytotox-48hr

Name: Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
Source: NCGC
External Id: TRND-SARS-CoV-2-PP

Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OPM1-m4-1

Total 139, Current Page 1 of 14

Taladegib

4-Fluoro-N-methyl-N-{1-[4-(1-methyl-1H-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl}-2-(trifluoromethyl)benzamide

LY 2940680

LY2940680

4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: LY2940680
Price: Check
Purity: 99.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: LY2940680
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Delivery: Inquiry
Contact: Ms Wang
Email: enquiry@dycnchem.com

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Price: $149/10mM*1mLinDMSO

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LY2940680

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Precursor & DownStream

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.