製品番号: HY-132302

Hu7691

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Based on 1 Customer Validation

Hu7691 is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.

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純度: 99.91%
CAS 番号: 2360523-76-6
分子式: C₂₂H₂₂ClF₃N₄O
分子量:450.88

保管条件:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Hu7691 構造式

CAS 番号: 2360523-76-6

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価格（税別）

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数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
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]

Akt1

4.0 nM (IC₅₀)

Akt2

97.5 nM (IC₅₀)

Akt3

28 nM (IC₅₀)

PKA

11 nM (IC₅₀)

PKCη

629 nM (IC₅₀)

ROCK1

354 nM (IC₅₀)

RSK1

756 nM (IC₅₀)

p70S6K

229 nM (IC₅₀)

Akt アイソフォーム固有の製品をすべて表示 :

PKA アイソフォーム固有の製品をすべて表示 :

PKC アイソフォーム固有の製品をすべて表示 :

ROCK アイソフォーム固有の製品をすべて表示 :

Ribosomal S6 Kinase (RSK) アイソフォーム固有の製品をすべて表示 :

SGK 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
769-P	IC₅₀	7.76 μM Compound: B5; Hu7691	Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
786-0	IC₅₀	2.5 μM Compound: B5; Hu7691	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
786-0	IC₅₀	8.6 μM Compound: B5; Hu7691	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
A549	IC₅₀	6.56 μM Compound: B5; Hu7691	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
Bel-7402	IC₅₀	26.62 μM Compound: B5; Hu7691	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
HaCaT	IC₅₀	15.17 μM Compound: B5; Hu7691	Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
HepG2	IC₅₀	3.6 μM Compound: B5; Hu7691	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
HGC-27	IC₅₀	0.68 μM Compound: B5; Hu7691	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
HT-29	IC₅₀	20.29 μM Compound: B5; Hu7691	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
KHOS/NP	IC₅₀	14.86 μM Compound: B5; Hu7691	Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
KHOS/NP	IC₅₀	7.47 μM Compound: B5; Hu7691	Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
L02	IC₅₀	5.4 μM Compound: B5; Hu7691	Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
LNCaP	IC₅₀	0.61 μM Compound: B5; Hu7691	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
MDA-MB-231	IC₅₀	16.37 μM Compound: B5; Hu7691	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
NCI-H1975	IC₅₀	7.56 μM Compound: B5; Hu7691	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
OS-RC-2	IC₅₀	9.9 μM Compound: B5; Hu7691	Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
OVCAR-8	IC₅₀	3.52 μM Compound: B5; Hu7691	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
PC-3	IC₅₀	8.74 μM Compound: B5; Hu7691	Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
SK-OV-3	IC₅₀	4.71 μM Compound: B5; Hu7691	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
SMMC-7721	IC₅₀	19.76 μM Compound: B5; Hu7691	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
U-251	IC₅₀	6.53 μM Compound: B5; Hu7691	Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
U-87MG ATCC	IC₅₀	9.26 μM Compound: B5; Hu7691	Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]

体外実験

Hu7691 displays low inhibitions against most of the kinases in the four families (AGC, TK, TKL, Lipid/Atypical; PKA, IC₅₀=11 nM; PKCη, IC₅₀=629 nM; ROCK1, IC₅₀=354 nM; RSK1, IC₅₀=756 nM; P70S6K, IC₅₀=229 nM; SGK, IC₅₀=1009 nM)^[1].
Hu7691 (2.25-36 μM; 24 hours) induces effective decrease of the phosphorylation level of Akt (S473)^[1].
B5 (10, 20, 30, 40 μM; for 72 h) exhibits low toxicity against HaCaT cells with an IC₅₀ value of 15.2 μM^[1].
Hu7691 has a significant inhibitory effect on the growth of 18 kinds of human tumor cells (U87-MG, U251, A549, HepG2, HT-29, KHOS, MDA-MB-231, PC3, SKOV3 and so on) derived from different tissues, with the IC₅₀ range of 0.6-27 μM. Hu7691 shows low antiproliferation activities against the HL7702 and HPDE6-C7 normal cells, exhibiting IC₅₀ values of 5.4 and 16.1 μM, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

HaCaT cells
Concentration:

2.25, 4.5, 9, 18, 36 μM
Incubation Time:

24 hours
Result:

Induced effective decrease of the phosphorylation level of Akt (S473).

体内実験

Hu7691 (12.5-50 mg/kg/day; i.g.; for 22 days) shows dose-dependent tumor growth inhibition^[1].
Hu7691 (15 mg/kg; oral) has a T_1/2 of 8.68 hours, a C_max of 171.17 ng/mL and an AUC of 2820.64 ng/mL h in rats^[1].
Hu7691 (2 mg/kg; iv) has a T_1/2 of 6.24 hours, a C_max of 207.52 ng/mL and an AUC of 532.87 ng/mL h in rats^[1].
Hu7691 (20 mg/kg; oral) has a T_1/2 of 16.7 hours, a C_max of 905.65 ng/mL and an AUC of 36303 ng/mL h in beagle dog (male, 40 weeks old, 8-10 kg)^[1].

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

Animal Model:

Balb/c mice (nu/nu, female, 3-4 weeks old, 20-25 g) with 786-O and KHOS xenograft^[1]
Dosage:

12.5, 25, 50 mg/kg
Administration:

Oral; once daily for 22 days
Result:

Showed dose-dependent tumor growth inhibition.

Animal Model:

SD rats (male, 8 weeks old, 250-300 g)^[1]
Dosage:

15 mg/kg (Pharmacokinetic Analysis)
Administration:

Oral
Result:

Had a T_1/2 of 8.68 hours, a C_max of 171.17 ng/mL and an AUC of 2820.64 ng/mL•h.

化学情報

CAS 番号 2360523-76-6
性状 Solid
分子量 450.88
分子式 C₂₂H₂₂ClF₃N₄O
Color White to off-white
SMILES

O=C(N[C@@H]1CNCC[C@H]1C2=CC=C(F)C(F)=C2)C3=CC=C(C4=CC=NN4C)C=C3F.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (221.79 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

2.2179 mL

11.0894 mL

22.1789 mL

5 mM

0.4436 mL

2.2179 mL

4.4358 mL

10 mM

0.2218 mL

1.1089 mL

2.2179 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 5 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.09 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 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)
μL
Number of Animals Number of Animals

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.
%
+
+
%
Tween-80 + +
%
Saline +

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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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Jinxin Che, et al. Discovery of N-((3 S,4 S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1 H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. J Med Chem. 2021 Aug 26;64(16):12163-12180. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2179 mL	11.0894 mL	22.1789 mL	55.4471 mL
	5 mM	0.4436 mL	2.2179 mL	4.4358 mL	11.0894 mL
	10 mM	0.2218 mL	1.1089 mL	2.2179 mL	5.5447 mL
	15 mM	0.1479 mL	0.7393 mL	1.4786 mL	3.6965 mL
	20 mM	0.1109 mL	0.5545 mL	1.1089 mL	2.7724 mL
	25 mM	0.0887 mL	0.4436 mL	0.8872 mL	2.2179 mL
	30 mM	0.0739 mL	0.3696 mL	0.7393 mL	1.8482 mL
	40 mM	0.0554 mL	0.2772 mL	0.5545 mL	1.3862 mL
	50 mM	0.0444 mL	0.2218 mL	0.4436 mL	1.1089 mL
	60 mM	0.0370 mL	0.1848 mL	0.3696 mL	0.9241 mL
	80 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6931 mL
	100 mM	0.0222 mL	0.1109 mL	0.2218 mL	0.5545 mL

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Hu7691

MCE Bioactive Compound Library

Akt アイソフォーム固有の製品をすべて表示

PKA アイソフォーム固有の製品をすべて表示

PKC アイソフォーム固有の製品をすべて表示

ROCK アイソフォーム固有の製品をすべて表示

Ribosomal S6 Kinase (RSK) アイソフォーム固有の製品をすべて表示

SGK 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

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

Hu7691 関連分類

HY-132302 関連分類