1. Stem Cell/Wnt
  2. Smo
  3. Taladegib

Taladegib (Synonyms: LY2940680)

Cat. No.: HY-13242 Purity: 99.76%
Handling Instructions

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

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

Taladegib Chemical Structure

Taladegib Chemical Structure

CAS No. : 1258861-20-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 149 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & 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].

Clinical Trial
Molecular Weight

512.50

Formula

C₂₆H₂₄F₄N₆O

CAS No.

1258861-20-9

SMILES

CN1N=CC=C1C2=C3C(C=CC=C3)=C(N=N2)N4CCC(CC4)N(C)C(C5=C(C=C(C=C5)F)C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (97.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9512 mL 9.7561 mL 19.5122 mL
5 mM 0.3902 mL 1.9512 mL 3.9024 mL
10 mM 0.1951 mL 0.9756 mL 1.9512 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Taladegib
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