Selinexor (KPT-330)

製品コードS7252 バッチS725205

化学情報

	Synonyms	ATG-010	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₁F₆N₇O
	分子量	443.31	CAS No.	1393477-72-9
Solubility (25°C)*	体外	DMSO	89 mg/mL (200.76 mM)
		Ethanol	89 mg/mL (200.76 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	Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2.
in vitro	As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM. ^[1]
in vivo	KPT-330 dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells. ^[1] In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines
	濃度	~1 μM
	反応時間	72 hours
	実験の流れ	Cell lines are cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum and penicillin/streptomycin. Cell Titer Glo assay is used to assess cell viability upon treatment with either dimethyl sulfoxide (DMSO) or KPT-330. Cells are plated at a density of 10 000 cells per well in a 96-well plate and incubated with DMSO or increasing concentrations of KPT-330. The cell viability is measured after 72 h exposure to KPT-330 and reported as a percentage of DMSO control cells. Jurkat cells that overexpress BCL2 are generated using MSCV-IRES-GFP retroviral expression system. Jurkat cells infected with BCL2 or control vector viruses are sorted by flow cytometry and the expression of BCL2 confirmed by Western blot analysis using BCL2 antibody.
動物実験	動物モデル	T-ALL and AML orthograft mouse model
	投薬量	20 -25 mg/kg
	投与方法	p.o.

参考

カスタマーフィードバック

: , , Mol Cancer Ther, 2017, 16(4):717-728

: Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.13886]

: Data from [Data independently produced by , , BMC Cancer, 2018, 18(1):764]

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：

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]	PubMed: 38262581
p300 nucleocytoplasmic shuttling underlies mTORC1 hyperactivation in Hutchinson-Gilford progeria syndrome [ Nat Cell Biol, 2024, 10.1038/s41556-023-01338-y]	PubMed: 38267537
Androgen deprivation induces double-null prostate cancer via aberrant nuclear export and ribosomal biogenesis through HGF and Wnt activation [ Nat Commun, 2024, 15(1):1231]	PubMed: 38336745
UCHL1 is a potential molecular indicator and therapeutic target for neuroendocrine carcinomas [ Cell Rep Med, 2024, S2666-3791(23)00610-9]	PubMed: 38244540
Phase-separated nuclear bodies of nucleoporin fusions promote condensation of MLL1/CRM1 and rearrangement of 3D genome structure [ Cell Rep, 2023, 42(8):112884]	PubMed: 37516964
KPT330 promotes the sensitivity of glioblastoma to olaparib by retaining SQSTM1 in the nucleus and disrupting lysosomal function [ Autophagy, 2023, 1-16.]	PubMed: 37712615
Nuclear export inhibition jumbles epithelial-mesenchymal states and gives rise to migratory disorder in healthy epithelia [ Elife, 2023, 12e81048]	PubMed: 36805020
Exportin 1-mediated nuclear/cytoplasmic trafficking controls drug sensitivity of classical Hodgkin's lymphoma [ Mol Oncol, 2023, 10.1002/1878-0261.13386]	PubMed: 36727672
Cytoplasmic Expression of TP53INP2 Modulated by Demethylase FTO and Mutant NPM1 Promotes Autophagy in Leukemia Cells [ Int J Mol Sci, 2023, 24(2)1624]	PubMed: 36675134
Azacitidine Is Synergistically Lethal with XPO1 Inhibitor Selinexor in Acute Myeloid Leukemia by Targeting XPO1/eIF4E/c-MYC Signaling [ Int J Mol Sci, 2023, 24(7)6816]	PubMed: 37047788

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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