CAY10566

製品番号: HY-15823 純度: 99.93%: Data Sheet SDS COA 取扱説明書
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CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC₅₀s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC₅₀=7.9 nM or 6.8 nM).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 944808-88-2

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$60	在庫あり	Estimated Time of Arrival: December 31
5 mg	$180	在庫あり	Estimated Time of Arrival: December 31
10 mg	$270	在庫あり	Estimated Time of Arrival: December 31
25 mg	$486	在庫あり	Estimated Time of Arrival: December 31
50 mg	$680	在庫あり	Estimated Time of Arrival: December 31
100 mg	$952	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1904	在庫あり	Estimated Time of Arrival: December 31
1 g	$2950	在庫あり	Estimated Time of Arrival: December 31
5 g		お問い合わせ
10 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 18 publication(s) in Google Scholar

顧客検証

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119. [Abstract]; XBP1 splicing in OVCAR-5 cells cultured in low-serum conditions and treated with SCD inhibitor CAY10566 (0-24.3 nM) for 48 h.

: CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119. [Abstract]; XBP1 splicing in primary cells from tumors of OC patients cultured in low-serum conditions and treated with 3 μM CAY10566 for 48 h or with 1 μM CAY10566 and 50 μM PA for 12 h.

: CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119. [Abstract]; XBP1 splicing in OVCAR-5 cells cultured in medium containing low serum and treated with 21.6 nM CAY10566 and indicated doses of OA for 48 h.

: CAY10566 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Jan;38:101807. [Abstract]; FBW7 silencing PANC-1 and SW1990 cells were treated with RSL3 (2 μmol/L) or CAY10566 (5 μmol/L) for 48–72 h and then detected cell viability.

: CAY10566 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Jan;38:101807. [Abstract]; TEM imaging was conducted in FBW7T205A overexpressed PANC-1 cells. RSL3 (2 μmol/L) and CAY10566 (5 μmol/L) treated PANC-1 cells functioned as the positive control. Red arrows showed the shrunken mitochondria. Blue arrows showed lipid droplets. The values below the western blot band represent the relative mean gray values of three independent experiments. Gray values were calculated by Adobe Photoshop CS6.

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製品説明

IC₅₀ & Target

IC50: 4.5 nM (SCD1 in mouse), 26 nM (SCD1 in human)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1155	IC₅₀	<10 nM Compound: 4	Inhibition of SCD in human NCI-H1155 cells non-expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay Inhibition of SCD in human NCI-H1155 cells non-expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay	[PMID: 32787093]
NCI-H2122	IC₅₀	<10 nM Compound: 4	Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay	[PMID: 32787093]

体外実験

CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation^[3].

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

Cell Proliferation Assay^[3]

Cell Line:	Swiss 3T3 cells
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	24 hours
Result:	Swiss 3T3 cell proliferation was concentration-dependently decreased.

体内実験

After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)^[4].

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

分子量

389.81

分子式

C₁₈H₁₇ClFN₅O₂

CAS 番号

944808-88-2

Appearance

Solid

Color

White to yellow

SMILES

CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1

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	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (64.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Acetone : 10 mg/mL (25.65 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5654 mL	12.8268 mL	25.6535 mL
5 mM	0.5131 mL	2.5654 mL	5.1307 mL
10 mM	0.2565 mL	1.2827 mL	2.5654 mL

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.34 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (274 KB) SDS (393 KB)

COA (246 KB) HNMR (240 KB) LCMS (367 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Masuda M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res. 2012 Aug;53(8):1543-52. [Content Brief]

[2]. Liu G, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem. 2007 Jun 28;50(13):3086-100. [Content Brief]

[3]. Koeberle A, et al. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol. J Biol Chem. 2012 Aug 3;287(32):27244-54. [Content Brief]

[4]. Kamphorst JJ, et al. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids. Proc Natl Acad Sci U S A. 2013 May 28;110(22):8882-7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Acetone / DMSO	1 mM	2.5654 mL	12.8268 mL	25.6535 mL	64.1338 mL
	5 mM	0.5131 mL	2.5654 mL	5.1307 mL	12.8268 mL
	10 mM	0.2565 mL	1.2827 mL	2.5654 mL	6.4134 mL
	15 mM	0.1710 mL	0.8551 mL	1.7102 mL	4.2756 mL
	20 mM	0.1283 mL	0.6413 mL	1.2827 mL	3.2067 mL
	25 mM	0.1026 mL	0.5131 mL	1.0261 mL	2.5654 mL
DMSO	30 mM	0.0855 mL	0.4276 mL	0.8551 mL	2.1378 mL
	40 mM	0.0641 mL	0.3207 mL	0.6413 mL	1.6033 mL
	50 mM	0.0513 mL	0.2565 mL	0.5131 mL	1.2827 mL
	60 mM	0.0428 mL	0.2138 mL	0.4276 mL	1.0689 mL

CAY10566 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

Keywords:

CAY10566944808-88-2CAY 10566CAY-10566Stearoyl-CoA Desaturase (SCD)Inhibitorinhibitorinhibit

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CAY10566

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CAY10566 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

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生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

CAY10566 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CAY10566 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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最近チェックした製品:

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