PIK-75

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PIK-75

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

372196-67-3

PIK-75 是一种可逆的DNA-PK和p110α-选择性的抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC₅₀分别为 2，5.8 和 76 nM。PIK-75 抑制 p110α 效果比抑制 p110β (IC₅₀=1.3 μM) 高 200 多倍。PIK-75 诱导凋亡 (apoptosis)。

生物活性

PIK-75 is a reversibleDNA-PKandp110α-selective inhibitor, which inhibitsDNA-PK, p110α and p110γ withIC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM)^[1]^[2]. PIK-75 inducesapoptosis^[3].

IC₅₀& Target

p110α

5.8 nM (IC₅₀)

p110γ

76 nM (IC₅₀)

p110δ

510 nM (IC₅₀)

p110β

1.3 μM (IC₅₀)

hsVPS34

2.6 μM (IC₅₀)

PI3KC2β

1 μM (IC₅₀)

PI3KC2α

10 μM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

ATM

2.3 μM (IC₅₀)

ATR

21 μM (IC₅₀)

mTORC1

1 μM (IC₅₀)

mTORC2

10 μM (IC₅₀)

DNA-PK

2 nM (IC₅₀)

体外研究
(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^[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC₅₀values of 1.2 and 1.3 μM, respectively^[1].
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 IC₅₀of 78 nM^[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death^[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells^[3].

Cell Viability Assay^[3]

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^[2]

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^[3].

体内研究
(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^[3].

Animal Model:	Mice bearing tumors of MIA PaCa-2^[3]
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.

分子量

452.28

Formula

C₁₆H₁₄BrN₅O₄S

CAS 号

372196-67-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.