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Selinexor(KPT-330)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Selinexor(KPT-330)图片
CAS NO:1393477-72-9
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)443.31
FormulaC17H11F6N7O
CAS No.1393477-72-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 89 mg/mL (200.8 mM)
Water: <1 mg/mL
Ethanol: 40 mg/mL (90.2 mM)
Solubility (In vivo)2% DMSO+49% PEG 300+dd H2O: 5mg/mL
Synonyms

KPT-330; KPT 330; KPT330

Chemical Name: (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide

SMILES Code: O=C(NNC1=NC=CN=C1)/C=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2

Exact Mass: 443.09293

实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: 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.

In VivoKPT-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. 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.
Animal modelT-ALL and AML orthograft mouse model
Formulation & Dosage Formulated in Pluronic F-68/PVP-K29/32; 20 -25 mg/kg; oral gavage
References

Br J Haematol. 2013 Apr;161(1):117-27; Leukemia. 2014 Jan;28(1):155-65.