Taladegib (LY2940680)

Catalog No.S2157

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

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Taladegib (LY2940680) Chemical Structure

Taladegib (LY2940680) Chemical Structure
Molecular Weight: 512.5

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Taladegib (LY2940680) is available in the following compound libraries:

Hedgehog/Smoothened Inhibitors with Unique Features

  • Selective Smoothened inhibitor

    PF-5274857 Smoothened-selective, IC50=5.8 nM.

  • Smoothened Inhibitor in Clinical Trial

    LDE225 (NVP-LDE225,Erismodegib) Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).

  • Newest Smoothened Inhibitor

    GANT61 Inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Smoothened Activator

    Purmorphamine Directly binds and activates Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM.

Product Information

  • Compare Hedgehog/Smoothened Inhibitors
    Compare Hedgehog/Smoothened Products
  • Research Area

Product Description

Biological Activity

Description Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
Targets Smoothened [1]
In vitro LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. [1]
In vivo LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. [2]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Redmond EM et al. Expert Opin Investig Drugs, 2011, 20(12),1649-1664.

[2] Mark H. Bender, Cancer Research, 2011, Volume 71, Issue 8, Supplement1

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02530437 Not yet recruiting Esophageal Cancer M.D. Anderson Cancer Center|National Cancer Institute (NC  ...more M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Eli Lilly and Company November 2016 Phase 1|Phase 2
NCT01919398 Recruiting Neoplasm Metastasis Eli Lilly and Company August 2013 Phase 1
NCT01697514 Withdrawn Medulloblastoma, Childhood|Rhabdomyosarcoma Eli Lilly and Company July 2013 Phase 1
NCT01722292 Terminated Small Cell Lung Carcinoma Eli Lilly and Company January 2013 Phase 1|Phase 2
NCT01746745 Completed Healthy Volunteers Eli Lilly and Company January 2013 Phase 1

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Chemical Information

Download Taladegib (LY2940680) SDF
Molecular Weight (MW) 512.5
Formula

C26H24F4N6O

CAS No. 1258861-20-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 0.66 mg/mL (1.28 mM)
Ethanol 2 mg/mL (3.9 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Hedgehog/Smoothened Products

  • Smoothened Agonist (SAG) HCl

    Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

  • SB225002

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

  • SB-334867

    SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

  • Vismodegib (GDC-0449)

    Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.

  • Cyclopamine

    Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

  • GANT61

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Purmorphamine

    Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

  • LDE225 (NVP-LDE225,Erismodegib)

    LDE225 (NVP-LDE225,Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

  • Glasdegib (PF-04449913)

    Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

  • SANT-1

    SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

    Features:Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.

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