A potent

PF-05212384 – 5 mg

Brand:
Cayman
CAS:
1197160-78-3
Storage:
-20
UN-No:
Non-Hazardous - /

Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.{15415,27164} PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).{29095,29096} It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.{29095,29096} PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).{29089} PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.{29088,29094}  

 

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Description

A potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR); active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously

Formal name: N-[4-[[4-(dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N’-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-urea

Synonyms:  PK-1587|PKI-587

Molecular weight: 615.7

CAS: 1197160-78-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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