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VER-246608

SKU: orb1218659

Description

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. VER-246608 was found to potentiate the activity of doxorubicin.

Images & Validation

Key Properties

CAS Number1684386-71-7
MW552.96
Purity>98% (HPLC)
FormulaC28H23ClF2N4O4
SMILESO=C(C1=CC=C(O)C=C1O)N(CC2=CC=C(CNC(C(F)F)=O)C=C2)C(C=C3)=CC=C3C4=NC(Cl)=NC=C4C
TargetPDK
SolubilityDMSO:100 mg/mL (180.84 mM; Need ultrasonic)

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information

VER-246608 (orb1218659)

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% DMSO +
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% Tween 80 +
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Available Sizes

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200 mg
500 mg
2 mg
$ 120.00
5 mg
$ 180.00
10 mg
$ 260.00
25 mg
$ 480.00
50 mg
$ 710.00
100 mg
$ 1,010.00