A selective PKM2 activator
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Product Categories

Product Type

Small Molecule Modulators
Small Molecule Activators
Kinases

Research Area

Cancer

ML-265

Item No. 13942

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2’,3’:4,5]pyrrolo[2,3-d]pyridazin-5-one
CAS Number
1221186-53-3
Synonyms
  • CID-44246499
  • NCGC00186528
  • TEPP-46
Molecular Formula
C17H16N4O2S2
Formula Weight
372.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
269, 304 nm
SMILES
CS(C1=CC(N2C)=C(S1)C3=C2C(N(CC4=CC(N)=CC=C4)N=C3)=O)=O
InChi Code
InChI=1S/C17H16N4O2S2/c1-20-13-7-14(25(2)23)24-16(13)12-8-19-21(17(22)15(12)20)9-10-4-3-5-11(18)6-10/h3-8H,9,18H2,1-2H3
InChi Key
ZWKJWVSEDISQIS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $129

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    25 mg

    $251

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    Cayman Chemical
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    Product Description

    ML-265 activates tumor-specific PKM2 (EC50 = 92 nM) by binding to the dimer-dimer interface between two subunits of PKM2 and inducing tetramerization, which is the most active form of the enzyme.1 It demonstrates >100-fold selectivity for PKM2 over the related PKM1, PKR, and PKL isoforms.1 At 50 mg/kg, ML-265 has been shown to reduce tumor size, weight, and occurrence in mice bearing H1299 cell xenografts in a model of human non-small cell lung carcinoma.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walsh, M.J., Brimacombe, K.R., Anastasiou, D., et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. Probe Reports from the NIH Molecular Libraries Program 1-21 (2012).