製品番号: HY-13260

CCT128930

7 Cited Publications

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

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.

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純度: 98.95%
CAS 番号: 885499-61-6
分子式: C₁₈H₂₀ClN₅
分子量:341.84

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CCT128930 構造式

CAS 番号: 885499-61-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (7)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

Akt2

6 nM (IC₅₀)

p70S6K

120 nM (IC₅₀)

PKA

168 nM (IC₅₀)

Autophagy

Apoptosis

Akt アイソフォーム固有の製品をすべて表示 :

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	0.66 μM Compound: 25	Inhibition of PIK-PKB-mTOR pathway in human PC3M cells Inhibition of PIK-PKB-mTOR pathway in human PC3M cells	[PMID: 18345609]
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	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	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]
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	IC₅₀	0.66 μM Compound: 25	Inhibition of PIK-PKB-mTOR pathway in human U87MG cells Inhibition of PIK-PKB-mTOR pathway in human U87MG cells	[PMID: 18345609]
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]

体外実験

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].

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

体内実験

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	T_1/2 (h)	T_max (h)	C_max (μM)	V_ss (L)	Cl (L/h)	AUC_0-∞ (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.

MedChemExpress (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.

化学情報

CAS 番号 885499-61-6
性状 Solid
分子量 341.84
分子式 C₁₈H₂₀ClN₅
Color Off-white to yellow
SMILES

ClC1=CC=C(C=C1)CC2(CCN(CC2)C3=NC=NC4=C3C=CN4)N
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All Bio/Physico-chemical AssayCell Proliferation/Viability AssayWBELISAIF

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Journal Impact Factor

Cell Death Dis

PEBP4 alleviates muscle wasting in lung cancer cachexia via KEAP1-NRF2-mediated redox homeostasis. [Abstract]

2026 Jun 3. PMID: 42236665
J Transl Med

Trained immunity attenuated acute lung injury by activating alveolar macrophages via AKT2-PDK1 axis-mediated metabolic reprogramming. [Abstract]

2025 Dec 23;23(1):1412. PMID: 41437043

CCT128930 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412. [Abstract]

Lactate secretion levels were measured following CCT128930 (CCT) treatment and compared with the TI group.

CCT128930 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412. [Abstract]

CCK-8 assay demonstrated reduced cellular lactate tolerance after CCT128930 (CCT) treatment.

CCT128930 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412. [Abstract]

Western blot and QPCR analyses revealed decreased PDK1 and inflammatory marker expression after CCT128930 (CCT) treatment.

CCT128930 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412. [Abstract]

TNF-α ELISA showed significant reduction after CCT128930 (CCT) treatment.

CCT128930 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412. [Abstract]

CCT128930 (CCT) treatment impaired phagocytic capacity.
Mol Cancer Ther

AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]

2024 Oct 1;23(10):1404-1417. PMID: 38894678
Biochem Biophys Res Commun

CCT128930 is a novel and potent antagonist of TRPM7 channel. [Abstract]

2021 Jun 30:560:132-138. PMID: 33989904
Patent

US20240066113A1.
J Healthc Eng

Study on Toll-Like Receptor 2-Mediated Inflammation-Induced Familial Hypertension Combined with Hyperlipemia and Its Mechanism. [Abstract]

2022 Jan 5:2022:1473597. PMID: 35035808
Oncotarget

Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML. [Abstract]

2016 May 17;7(20):29131-42. PMID: 27074558

溶剤 & 溶解度

体外:

DMSO : 33.33 mg/mL (97.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9253 mL

14.6267 mL

29.2535 mL

5 mM

0.5851 mL

2.9253 mL

5.8507 mL

10 mM

0.2925 mL

1.4627 mL

2.9253 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
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+
%
Tween-80 + +
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. Yap TA et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71. [Content Brief]

[2]. Wang FZ, et al. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. Biochimie. 2014;103:118-125. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

CCT128930

7 Cited Publications

100 mg お問い合わせ

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CCT128930

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

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Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 CCT128930

Akt アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

CCT128930 関連分類

HY-13260 関連分類