KPT-185

製品コードS7125 バッチS712501

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
* <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. KPT-185 reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. ^[1] KPT-185 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. KPT-185 reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. ^[1] KPT-185 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

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：

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。

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