CH5132799

CH5132799

CAT N°: 26410
Price:

From 299.00 254.15

CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3K?, PI3K?, PI3K?, and PI3K?, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2? and PI3KC2?, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3K?H1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-pyrimidinamine
  • Correlated keywords
    • 1431855-32-1 CH-5132799 5137291 PA799 PI3K-? ?H1047R ? ? ? C2? C2? Vps-34 HCT-116 KPL4 T-47D SKOV-3 PC-3 PA-799 CH5137291
  • Product Overview:
    CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3K?, PI3K?, PI3K?, and PI3K?, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2? and PI3KC2?, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3K?H1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.

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