KPT-185

製品コードS7125 バッチS712502

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₆H₁₆F₃N₃O₃

分子量

355.31

CAS No.

1333151-73-7

Solubility (25°C)*

体外

DMSO

71 mg/mL (199.82 mM)

Ethanol

71 mg/mL (199.82 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.550mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.100mg/ml (3.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	KPT-185 is a selective CRM1 inhibitor that induces growth inhibition and apoptosis in a panel of NHL cell lines with a median IC50 ~25 nM.
in vitro	KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts. This compound reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. ^[1] It also inhibits proliferation and promotes apoptosis of pancreatic cancer cells without affecting human pancreatic ductal epithelial cells. ^[2]

製品説明

KPT-185 is a selective CRM1 inhibitor that induces growth inhibition and apoptosis in a panel of NHL cell lines with a median IC50 ~25 nM.

in vitro

KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts. This compound reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. ^[1] It also inhibits proliferation and promotes apoptosis of pancreatic cancer cells without affecting human pancreatic ductal epithelial cells. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	AML cell lines (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1)
	濃度	~10 μM
	反応時間	72 hours
	実験の流れ	Cells are seeded into 96-well plates and treated for 24, 48, and 72 hours with KPT-SINE at various concentrations ranging from 10 nM to 10 μM. Cell viability is evaluated using the cell proliferation reagent WST-1 according to the manufacturer's protocol. The absorbance of wells at 450 nm (reference wavelength, 650 nm) is measured with a microplate reader.

参考

https://pubmed.ncbi.nlm.nih.gov/22677130/
https://pubmed.ncbi.nlm.nih.gov/23089203/

カスタマーフィードバック

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2018, 503(3):1544-1549]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inhibition of XPO1 by selinexor enhances terminal erythroid maturation through modulation of HSP70 trafficking in severe β0-thalassemia/HbE [ PLoS One, 2025, 20(9):e0333127]	PubMed: 40997022
Discovery of compounds that reactivate p53 mutants in vitro and in vivo [ Cell Chem Biol, 2022, S2451-9456(22)00275-6]	PubMed: 35948006
Targeted CRM1-inhibition perturbs leukemogenic NUP214 fusion proteins and exerts anti-cancer effects in leukemia cell lines with NUP214 rearrangements [ Oncotarget, 2020, 11(36):3371-3386]	PubMed: 32934780
STK38 kinase acts as XPO1 gatekeeper regulating the nuclear export of autophagy proteins and other cargoes [ EMBO Rep, 2019, 20(11):e48150]	PubMed: 31544310
NEDD4 protects vascular endothelial cells against Angiotensin II-induced cell death via enhancement of XPO1-mediated nuclear export. [ Exp Cell Res, 2019, 10.1016/j.yexcr.2019.111505]	PubMed: 31326389
XPO1-mediated nuclear export of RNF146 protects from angiotensin II-induced endothelial cellular injury [Sheng Z Biochem Biophys Res Commun, 2018, 503(3):1544-1549]	PubMed: 30029878
EGFR feedback-inhibition by Ran-binding protein 6 is disrupted in cancer. [ Nat Commun, 2017, 8(1):2035]	PubMed: 29229958
Inhibiting PLK1 induces autophagy of acute myeloid leukemia cells via mammalian target of rapamycin pathway dephosphorylation. [Tao YF, et al. Oncol Rep, 2017, 37(3):1419-1429]	PubMed: 28184925
Activation of Yap-Directed Transcription by Knockdown of Conserved Cellular Functions. [ J Biomol Screen, 2016, 21(3):269-76]	PubMed: 26637552

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。