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Taladegib

SKU: orb1305194

Description

Taladegib (LY2940680) is a potent, orally active smoothened (Smo) antagonist that inhibits the Hedgehog signaling pathway. It is used in cancer research, demonstrating antitumor activity in both in vitro assays and in vivo models of Hedgehog pathway-dependent malignancies.

Research Area

Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number1258861-20-9
MW512.5
Purity98.75% (May vary between batches)
FormulaC26H24F4N6O
SMILESCN(C1CCN(CC1)c1nnc(-c2ccnn2C)c2ccccc12)C(=O)c1ccc(F)cc1C(F)(F)F
TargetSmo,Hedgehog/Smoothened
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.95 mM);DMSO:5.64 mg/mL (11 mM)

Bioactivity

In Vivo
Taladegib has excellent pharmacokinetic properties in rodent and non-rodent species. Taladegib administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. Taladegib reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and Taladegib induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. Taladegib inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity.
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.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Inhibitor, Hedgehog, inhibit, LY2940680, LY-2940680, LY 2940680, Smo, Smoothened, Taladegib

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  • LY2940680 [orb1226657]

    >98% (HPLC)

    1258861-20-9

    512.502

    C26H24F4N6O

    2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 25 mg, 500 mg, 1 g
Quality Guarantee

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Key Properties

No computed properties available.

Protocol Information

Available Sizes

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2 mg
$ 80.00
5 mg
$ 100.00
10 mg
$ 130.00
25 mg
$ 200.00
50 mg
$ 290.00
100 mg
$ 400.00
200 mg
$ 540.00
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