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  2. PI3K/Akt/mTOR
  3. PI3K
  4. IPI-3063

IPI-3063 是一種有效的選擇性 PI3K p110δ 抑制劑，IC50 為 2.5±1.2 nM。

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IPI-3063 Chemical Structure

IPI-3063 Chemical Structure

CAS No. : 1425043-73-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1229
In-stock
1 mg ￥479
In-stock
2 mg ￥703
In-stock
5 mg ￥1226
In-stock
10 mg ￥2038
In-stock
25 mg ￥3350
In-stock
50 mg ￥4700
In-stock
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

生物活性

IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5?±?1.2 nM.

IC50 & Target[1]

p110δ

2.5 nM (IC50)

p110α

1170 nM (IC50)

p110β

1508 nM (IC50)

p110γ

2187 nM (IC50)

體外研究
(In Vitro)

IPI-3063 inhibits p110α, p110β, and p110γ with IC50s of 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1. IPI-3063 is a p110δ selective compound with an IC50=0.1?nM in p110δ-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are at least 1,000-fold higher (IC50=1901±1318 nM for p110α, IC50=102.8±35.7 nM for p110β, IC50=418.8±117.2 nM for p110γ). IPI-3063 is very potent in reducing p-AKT (significant effect at 1?nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10?nM. IPI-3063 is very potent, achieving a significant decrease in B cell survival when present at 10?nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

455.51

Formula

C25H25N7O2
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 62.5 mg/mL (137.21 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 2.1953 mL 10.9767 mL 21.9534 mL
5 mM 0.4391 mL 2.1953 mL 4.3907 mL
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料

純度: 99.22%

參考文獻
Kinase Assay
[1]

Human recombinant PI3K-α, PI3K-β, PI3K-δ, and PI3K-γ are used. Phosphatidylinositol 4,5 bis phosphate (diC8-PtdIns(4,5)P2) is used. PI3K-α, β, and δ are heterodimers consisting of full length p110α, p110β, or p110δ catalytic subunit and the p85α regulatory subunit. PI3K-γ is a monomer of the p110γ catalytic subunit. Samples of kinase (10?nM-α, β, and δ; 20?nM-γ) are incubated with IPI-3063 for 30?min at room temperature in reaction buffer (15?mM HEPES pH 7.4, 20?mM NaCl, 1?mM EGTA, 0.02% Tween 20, 10?mM MgCl2, 0.2?mg/mL bovine-γ-globulins) followed by addition of ATP/diC8-PtdIns(4,5)P2 mixture to give final concentrations of 3?mM ATP and 500?μM diC8-PtdIns(4,5)P2. Reactions are incubated at room temperature for 2?h, with PI3K activity is assessed. Plates are read on plate reader in luminescence mode[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Peripheral blood mononuclear cells (PBMCs) are first purified from blood by density gradient centrifugation. Human B cells are then purified from PBMCs by negative selection. B-cell purity is increased from 4% to >70% as measured by FACS analysis using anti-CD19 PE conjugated antibody. Purified B cells are seeded at a final concentration of 0.1×106?cells/mL and cultured with 2?μg/mL human CD40L+5?μg/mL anti-human IgM/IgG+100?μg/mL hIL-2+100?μg/mL hIL-21. All B cells are cultured in RPMI 1640 supplemented with 10% (vol/vol) heat-inactivated FCS, 5?mM Hepes, 2?mM L-glutamine, 100?U/mL Penicillin, 100?μg/mL Streptomycin, 50?μM 2-mercaptoethanol. Purified human B cells are pretreated with IPI-3063 (0.1, 1, 10, and 100?nM) for 30?min, then stimulated with human CD40L+anti-human IgM/IgG+human IL-2+human IL-21 for 120?h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1953 mL 10.9767 mL 21.9534 mL 54.8835 mL
5 mM 0.4391 mL 2.1953 mL 4.3907 mL 10.9767 mL
10 mM 0.2195 mL 1.0977 mL 2.1953 mL 5.4884 mL
15 mM 0.1464 mL 0.7318 mL 1.4636 mL 3.6589 mL
20 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
25 mM 0.0878 mL 0.4391 mL 0.8781 mL 2.1953 mL
30 mM 0.0732 mL 0.3659 mL 0.7318 mL 1.8295 mL
40 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
50 mM 0.0439 mL 0.2195 mL 0.4391 mL 1.0977 mL
60 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9147 mL
80 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6860 mL
100 mM 0.0220 mL 0.1098 mL 0.2195 mL 0.5488 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產品名稱：
IPI-3063
目錄號：
HY-111510
需求量：