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  2. PI3K/Akt/mTOR
  3. PI3K
  4. ETP-46321

ETP-46321 是一種有效的 PI3Kα 和 PI3Kδ 抑制劑，Kiapp 分別為 2.3 和 14.2 nM。

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ETP-46321 Chemical Structure

ETP-46321 Chemical Structure

CAS No. : 1252594-99-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
100 mg ￥7950
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.

IC50 & Target[1]

p110α

2.3 nM (Ki)

PI3Kα-E545K

1.77 nM (Ki)

PI3Kα-E542K

1.89 nM (Ki)

PI3Kα-H1047R

2.33 nM (Ki)

p110δ

14.2 nM (Ki)

p110β

170 nM (Ki)

p110γ

179 nM (Ki)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
U2OS IC50
8.3 nM
Compound: 14, ETP-46321
Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot
Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot
[PMID: 22520259]
體外研究
(In Vitro)

ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (Kiapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC50 of 8.3 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques[1].

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

473.55

Formula

C20H27N9O3S
CAS 號
性狀

固體

顏色

White to off-white

運(yùn)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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 33 mg/mL (69.69 mM; 吸濕的 DMSO 對產(chǎn)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(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1117 mL 10.5585 mL 21.1171 mL
5 mM 0.4223 mL 2.1117 mL 4.2234 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)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(jì)算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Animal Administration
[1]

Mice[1]
BALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.

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

完整儲備液配制表

* 請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1117 mL 10.5585 mL 21.1171 mL 52.7927 mL
5 mM 0.4223 mL 2.1117 mL 4.2234 mL 10.5585 mL
10 mM 0.2112 mL 1.0559 mL 2.1117 mL 5.2793 mL
15 mM 0.1408 mL 0.7039 mL 1.4078 mL 3.5195 mL
20 mM 0.1056 mL 0.5279 mL 1.0559 mL 2.6396 mL
25 mM 0.0845 mL 0.4223 mL 0.8447 mL 2.1117 mL
30 mM 0.0704 mL 0.3520 mL 0.7039 mL 1.7598 mL
40 mM 0.0528 mL 0.2640 mL 0.5279 mL 1.3198 mL
50 mM 0.0422 mL 0.2112 mL 0.4223 mL 1.0559 mL
60 mM 0.0352 mL 0.1760 mL 0.3520 mL 0.8799 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(chǎn)品名稱：
ETP-46321
目錄號：
HY-12340
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