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  2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. Akt Autophagy Apoptosis
  4. CCT128930

CCT128930 是一種 ATP 競爭性地且選擇性的 AKT 抑制劑 (對AKT2 的 IC50 為 6 nM )。CCT128930 通過靶向 AKT 的 Met282 (PKA-AKT嵌合體的 Met173)，對 PKA 激酶 (IC50=168 nM) 具有 28 倍的選擇性，對 p70S6K (IC50=120 nM) 具有 20 倍的選擇性。具有抗腫瘤活性。

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CCT128930 Chemical Structure

CCT128930 Chemical Structure

CAS No. : 885499-61-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1072
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1 mg ￥550
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5 mg ￥975
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10 mg ￥1560
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50 mg ￥5000
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100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
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查看 Akt 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.

IC50 & Target[1]

Akt2

6 nM (IC50)

p70S6K

120 nM (IC50)

PKA

168 nM (IC50)

Autophagy

 

Apoptosis

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
PC-3M GI50
12 nM
Compound: 2, CCT128930
Antiproliferative activity against human PC3M cells after 96 hrs by SRB assay
Antiproliferative activity against human PC3M cells after 96 hrs by SRB assay
[PMID: 20151677]
PC-3M IC50
12 μM
Compound: 25
Growth inhibition of human PC3M cells by SRB assay
Growth inhibition of human PC3M cells by SRB assay
[PMID: 18345609]
U-87MG ATCC IC50
0.66 nM
Compound: 2, CCT128930
Inhibition of PKB in human U87MG cells assessed as GSK3-beta phosphorylation by ELISA
Inhibition of PKB in human U87MG cells assessed as GSK3-beta phosphorylation by ELISA
[PMID: 20151677]
U-87MG ATCC IC50
0.66 μM
Compound: 25
Inhibition of GSK3-beta in human U87MG cells by ELISA
Inhibition of GSK3-beta in human U87MG cells by ELISA
[PMID: 18345609]
U-87MG ATCC GI50
5 nM
Compound: 2, CCT128930
Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay
Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay
[PMID: 20151677]
U-87MG ATCC IC50
5 μM
Compound: 25
Growth inhibition of human U87MG cells by SRB assay
Growth inhibition of human U87MG cells by SRB assay
[PMID: 18345609]
U-87MG ATCC GI50
6.3 μM
Compound: 14; CCT128930
Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay
Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay
[PMID: 30583248]
體外研究
(In Vitro)

The GI50 values of CCT128930 for growth inhibition are 6.3 μM for U87MG human glioblastoma cells, 0.35 μM for LNCaP human prostate cancer cells, and 1.9 μM for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines[1].
CCT128930 (0.1-60 μM; 1 hour; U87MG human glioblastoma cells) shows an initial induction of AKT phosphorylation at serine 473 up to 20 μM, followed by a decreased in phosphorylation at higher concentrations[1].
CCT128930 inhibits direct substrates of AKT (Ser9 GSK3β, pThr246 PRAS40 and pT24 FOXO1/p32 FOXO3a) at ≥5 μM, and the downstream target, pSer235/236 S6RP at ≥ 10 μM, with generally constant levels of the respective total proteins and GAPDH[1].
CCT128930 (18.9 μM; U87MG human glioblastoma cells) causes an increase in phosphorylation of pSer473 AKT after 30 minutes, which is sustained for 48 hours. Total AKT protein signal decreases gradually from 8 hours to 48 hours of treatment[1].
CCT128930 (PTEN-null U87MG human glioblastoma cells; over a 24-hour time period) results in an increase in G0/G1 phase cells from 43.6% to 64.8% after 24 hours of treatment[1].
CCT128930 (0-10 μM; 24 hours) increases, but not inhibites, the phosphorylation of Akt in HepG2 and A549 cells. CCT128930 (0-20 μM; 24 hours) inhibits cell proliferation by inducing cell cycle arrest in G1 phase through downregulation of cyclinD1 and Cdc25A, and upregulation of p21, p27 and p53. CCT128930 (20 μM) triggers cell apoptosis with activation of caspase-3, caspase-9, and PARP. CCT128930 (0-20 μM; 24 hours) increases phosphorylation of ERK and JNK in HepG2 cells. CCT128930 (0-20 μM; 24 hours) activates DNA damage response of HepG2 cell characterized by phosphorylation of H2AX, ATM (ataxia-telangiectasia mutated), Chk1 and Chk2[2].

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

CCT128930 (25 or 40 mg/kg; i.p. daily or twice daily for 5 days) shows antitumor activities in U87MG and BT474 human breast cancer xenografts[1].
Summary of the pharmacokinetic parameters of CCT128930 (25 mg/kg) in CrTacNCr-Fox1nu mice[1]

Tissue Route T1/2
(h)		 Tmax
(h)		 Cmax
(μM)		 Vss
(L)		 Cl
(L/h)		 AUC0-∞
(μMh)		 Bioavailability
(%)
Plasma i.v. 0.95 0.083 6.36 0.25 0.325 4.62 100
Plasma i.p. 2.33 0.5 1.28 N/A 0.372 1.33 28.8
Tumor i.p. 3.89 1 8.02 N/A 0.06* 25.8 N/A
Plasma p.o. 0.57 0.5 0.432 N/A 0.317 0.392 8.5

*Apparent clearance.

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

Animal Model: 6-8 weeks old female CrTacNCr-Fox1nu mice[1]
Dosage: 25 mg/kg (U87MG human glioblastoma xenografts) or 40 mg/kg (BT474 human breast cancer xenografts)
Administration: i.p. daily for 5 days (U87MG human glioblastoma xenografts); i.p. twice daily for 5 days (BT474 human breast cancer xenografts)
Result: Giving a treated:control (T/C) ratio on day 12 of 48%. There was no weight loss associated with this regime in U87MG human glioblastoma xenografts.
Had a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. This regimen was associated with minimal weight loss, with a nadir of only 94.8% of the initial body weight on day 15 of treatment in BT474 human breast cancer xenografts.
分子量

341.84

Formula

C18H20ClN5
CAS 號
性狀

固體

顏色

Off-white to yellow

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 : 33.33 mg/mL (97.50 mM; 超聲助溶 (<60°C); 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.9253 mL 14.6267 mL 29.2535 mL
5 mM 0.5851 mL 2.9253 mL 5.8507 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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.69%

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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，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 2.9253 mL 14.6267 mL 29.2535 mL 73.1336 mL
5 mM 0.5851 mL 2.9253 mL 5.8507 mL 14.6267 mL
10 mM 0.2925 mL 1.4627 mL 2.9253 mL 7.3134 mL
15 mM 0.1950 mL 0.9751 mL 1.9502 mL 4.8756 mL
20 mM 0.1463 mL 0.7313 mL 1.4627 mL 3.6567 mL
25 mM 0.1170 mL 0.5851 mL 1.1701 mL 2.9253 mL
30 mM 0.0975 mL 0.4876 mL 0.9751 mL 2.4378 mL
40 mM 0.0731 mL 0.3657 mL 0.7313 mL 1.8283 mL
50 mM 0.0585 mL 0.2925 mL 0.5851 mL 1.4627 mL
60 mM 0.0488 mL 0.2438 mL 0.4876 mL 1.2189 mL
80 mM 0.0366 mL 0.1828 mL 0.3657 mL 0.9142 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：
CCT128930
目錄號：
HY-13260
需求量：