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PIK75

SKU: orb1222313

Description

PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

Images & Validation

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PIK75

Key Properties

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CAS Number372196-67-3
MW452.28
Purity>98% (HPLC)
FormulaC16H14BrN5O4S
SMILESCC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br
TargetP450

Bioactivity

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In Vivo
PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) In vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice. Animal model: Mice bearing tumors of MIA PaCa-2. Dosage: 2 mg/kg; or combination with Gemcitabine (20 mg/kg). Administration: Administered injection; 5 times per week. 25 days. Result: Reduced the tumor growth and enhanced the antitumor effect.
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In Vitro
PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively. PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively. PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM. PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death. PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells. Cell Viability Assay Cell line: Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1). Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM Incubation time: 48 hours. Result: Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment. Western blot analysis. Cell line: Overnight-starved CHO-IR cells. Concentration: 1, 10, 100, 1000 nM. Incubation time: 5 minutes. Result: Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner. PIK-75 potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice.
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Storage & Handling

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

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  • PIK-75

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Gene Symbol
P450

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PIK75 (orb1222313)

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5 mg
$ 80.00
10 mg
$ 100.00
25 mg
$ 180.00
50 mg
$ 290.00
100 mg
$ 490.00
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