Eltanexor (Synonyms: KPT-8602)

Name: Eltanexor
Brand: MedChemExpress
SKU: HY-100423
Rating: 5.0 (3 reviews)

製品番号: HY-100423 純度: 99.79%: Data Sheet SDS COA 取扱説明書
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Technical Support

Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC₅₀=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines.

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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 : 1642300-52-4

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 316	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 316	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$75	在庫あり	Estimated Time of Arrival: December 31
5 mg	$288	在庫あり	Estimated Time of Arrival: December 31
10 mg	$340	在庫あり	Estimated Time of Arrival: December 31
25 mg	$545	在庫あり	Estimated Time of Arrival: December 31
50 mg	$800	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1160	在庫あり	Estimated Time of Arrival: December 31
500 mg	$2300	在庫あり	Estimated Time of Arrival: December 31
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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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Based on 3 publication(s) in Google Scholar

Other Forms of Eltanexor:

Eltanexor Z-isomer 在庫あり

顧客検証

Cell Proliferation/Viability Assay

RT-PCR

: Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112.; Eltanexor (0.05-0.8 μM) inhibited the expression of IE2/86 (encoded by UL122), early protein pp52 (UL44), and late proteins pp71 and pp65 (UL82 and UL83) in a dose-dependent manner in HFFs infected with HCMV.

: Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112.; Eltanexor (0.05-0.8 μM) inhibited the production of HCMV progeny virions in a dose-dependent manner.

: Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112.; Eltanexor (0.4 μM; 36-96 h) increaseed the transcript levels of UL36, and reduced the transcript levels of UL122, E (UL44) and L (UL82, UL83, UL99, and UL75) genes in HFFs infected with HCMV.

: Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112.; Eltanexor (0.4 μM; 6-96 h) significantly reduced IE2, and suppressesed the protein levels of E protein pp52 (encoded by UL44), pp65 (UL83), pp71 (UL82), and L protein pp28 (UL99) after 36 hpi in HFFs infected with HCMV.

: Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112.; Eltanexor (0.4 μM) inhibited the nuclear export of the viral tegument protein pp65 in HFFs infected with HCMV.

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製品説明

IC₅₀ & Target

XPO1^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MM1.S	IC₅₀	64 1 Compound: KPT-8602	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
H9	IC₅₀	139.4 1 Compound: KPT-8602	Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
H9	IC₅₀	139.4 1 Compound: KPT-8602	Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
MM1.S	IC₅₀	64 1 Compound: KPT-8602	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
NAMALVA	IC₅₀	93.8 1 Compound: KPT-8602	Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
MM1.S	IC₅₀	64 1 Compound: KPT-8602	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
YT	IC₅₀	103.1 1 Compound: KPT-8602	Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
NAMALVA	IC₅₀	93.8 1 Compound: KPT-8602	Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
NAMALVA	IC₅₀	93.8 1 Compound: KPT-8602	Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
YT	IC₅₀	103.1 1 Compound: KPT-8602	Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
H9	IC₅₀	139.4 1 Compound: KPT-8602	Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
YT	IC₅₀	103.1 1 Compound: KPT-8602	Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]

体外実験

KPT-8602 (2-6 nM; 72 hours) reduces cell viability in leukemia cell lines with EC₅₀s ranging from 25 to 145 nM^[1].
KPT-8602 (1 nM; 16 hours) induces apoptosis in leukemia cell lines^[1].

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

Cell Viability Assay^[1]

Cell Line:	T-ALL cells (Jurkat, MOLT-4, ALL-SIL, DND41, and HPB-ALL), B-ALL cells (BV173, EHEB, and REH), AML cells (MV4-11, MOLM13, K-562, and HL-60)
Concentration:	2, 4, 6 nM
Incubation Time:	72 hours
Result:	Cell viability was reduced with EC₅₀ values ranging from 25 to 145 nM.

Western Blot Analysis^[1]

Cell Line:	T-ALL, B-ALL, AML cells
Concentration:	1 μM
Incubation Time:	16 hours
Result:	Appearance of cleaved caspase-3 substrate PARP as early as 6 hours.

体内実験

KPT-8602 (15 mg/kg; oral gavage; daily for 12 days) shows potent anti-lymphoblastic leukemia activity^[1].

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

Animal Model:	Female BALB/c mice (model with the JAK3 (M511I) mutation)^[1]
Dosage:	15 mg/kg
Administration:	Oral gavage; daily for 12 days
Result:	Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12.

臨床実験

分子量

428.29

分子式

C₁₇H₁₀F₆N₆O

CAS 番号

1642300-52-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

FC(F)(F)C1=CC(C(F)(F)F)=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=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 : ≥ 100 mg/mL (233.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3349 mL	11.6743 mL	23.3487 mL
5 mM	0.4670 mL	2.3349 mL	4.6697 mL
10 mM	0.2335 mL	1.1674 mL	2.3349 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.84 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 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.84 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.84 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.

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: 99.84%

Select Batch:

データシート (279 KB) SDS (393 KB)

COA (252 KB) Elemental Analysis Report (110 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Vercruysse T et al. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.3349 mL	11.6743 mL	23.3487 mL	58.3717 mL
	5 mM	0.4670 mL	2.3349 mL	4.6697 mL	11.6743 mL
	10 mM	0.2335 mL	1.1674 mL	2.3349 mL	5.8372 mL
	15 mM	0.1557 mL	0.7783 mL	1.5566 mL	3.8914 mL
	20 mM	0.1167 mL	0.5837 mL	1.1674 mL	2.9186 mL
	25 mM	0.0934 mL	0.4670 mL	0.9339 mL	2.3349 mL
	30 mM	0.0778 mL	0.3891 mL	0.7783 mL	1.9457 mL
	40 mM	0.0584 mL	0.2919 mL	0.5837 mL	1.4593 mL
	50 mM	0.0467 mL	0.2335 mL	0.4670 mL	1.1674 mL
	60 mM	0.0389 mL	0.1946 mL	0.3891 mL	0.9729 mL
	80 mM	0.0292 mL	0.1459 mL	0.2919 mL	0.7296 mL
	100 mM	0.0233 mL	0.1167 mL	0.2335 mL	0.5837 mL

Eltanexor 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:

Eltanexor1642300-52-4KPT-8602KPT8602KPT 8602CRM1Chromosomal Maintenance 1Exportin 1XPO1Inhibitorinhibitorinhibit

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Eltanexor (Synonyms: KPT-8602)

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Other Forms of Eltanexor:

Eltanexor 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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•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

Eltanexor 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Eltanexor Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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