KPT-185

製品番号: HY-15611 純度: 99.04%: Data Sheet SDS COA 取扱説明書
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KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC₅₀=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts.

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。

KPT-185 構造式

CAS 番号 : 1333151-73-7

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 66	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$94	在庫あり	Estimated Time of Arrival: December 31
25 mg	$169	在庫あり	Estimated Time of Arrival: December 31
50 mg	$259	在庫あり	Estimated Time of Arrival: December 31
100 mg		お問い合わせ
200 mg		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.

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•関連タンパク質:

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

製品説明

IC₅₀ & Target

CRM1^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	EC₅₀	5 nM Compound: 14; KPT-185	Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay	[PMID: 39005064]

体外実験

KPT-185 results in a significant decrease in the level of CRM1 protein and a significant accumulation of p53 in the nucleus of MV4-11 and OCI-AML3 cells^[1].
KPT-185 (1-1000 nM; 72 hours) dramatically reduces HPB-ALL, Jurkat, CCRF-CEM, MOLT-4, KOPTK1, LOUCY cells growth with IC₅₀s of 16-395 nM^[4].
KPT-185 leads to cell cycle arrest in G1 phase in the MOLT-4 cell line^[4].

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

Cell Viability Assay^[4]

Cell Line:	HPB-ALL, Jurkat, CCRF-CEM, MOLT-4, KOPTK1, LOUCY cells
Concentration:	1, 10, 100, 1000 nM
Incubation Time:	72 hours
Result:	The growth of those lines was dramatically reduced with IC₅₀s of 16–395 nM after 72 h of exposure.

分子量

355.31

分子式

C₁₆H₁₆F₃N₃O₃

CAS 番号

1333151-73-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(OC(C)C)/C=C\N1N=C(C2=CC(C(F)(F)F)=CC(OC)=C2)N=C1

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 : 50 mg/mL (140.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (140.72 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8144 mL	14.0722 mL	28.1444 mL
5 mM	0.5629 mL	2.8144 mL	5.6289 mL
10 mM	0.2814 mL	1.4072 mL	2.8144 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, 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.

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 (7.04 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (7.04 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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.04 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 EtOH stock solution (25.0 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.
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: 99.04%

Select Batch:

データシート (275 KB) SDS (393 KB)

COA (250 KB) LCMS (97 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Ranganathan P, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120(9):1765-73. [Content Brief]

[2]. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activityin preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27. [Content Brief]

[3]. Zhang K, et al. Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma. Exp Hematol. 2013 Jan;41(1):67-78.e4. [Content Brief]

[4]. Salas Fragomeni RA, et al. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12(7):1171-9. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / Ethanol	1 mM	2.8144 mL	14.0722 mL	28.1444 mL	70.3611 mL
	5 mM	0.5629 mL	2.8144 mL	5.6289 mL	14.0722 mL
	10 mM	0.2814 mL	1.4072 mL	2.8144 mL	7.0361 mL
	15 mM	0.1876 mL	0.9381 mL	1.8763 mL	4.6907 mL
	20 mM	0.1407 mL	0.7036 mL	1.4072 mL	3.5181 mL
	25 mM	0.1126 mL	0.5629 mL	1.1258 mL	2.8144 mL
	30 mM	0.0938 mL	0.4691 mL	0.9381 mL	2.3454 mL
	40 mM	0.0704 mL	0.3518 mL	0.7036 mL	1.7590 mL
	50 mM	0.0563 mL	0.2814 mL	0.5629 mL	1.4072 mL
	60 mM	0.0469 mL	0.2345 mL	0.4691 mL	1.1727 mL
	80 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8795 mL
	100 mM	0.0281 mL	0.1407 mL	0.2814 mL	0.7036 mL

KPT-185 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:

KPT-1851333151-73-7KPT185KPT 185CRM1Chromosomal Maintenance 1Exportin 1XPO1Inhibitorinhibitorinhibit

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