Eltanexor(KPT-8602)

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Eltanexor(KPT-8602)

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。

CAS NO:

1642300-52-4

包装与价格：

包装	价格(元)
1mg	询价
5mg	询价
10mg	询价
50mg	询价

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	428.29
Cas No.	1642300-52-4
Formula	C₁₇H₁₀F₆N₆O
Solubility	insoluble in H2O; insoluble in EtOH; ≥44 mg/mL in DMSO
Chemical Name	(E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide
Canonical SMILES	FC(F)(F)C1=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=CC(C(F)(F)F)=C1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Eltanexor (KPT-8602) is a second-generation, orally bioavailable inhibitor of exportin 1 (XPO1), with IC50 values of 20 ~ 211 nM in 10 acute myeloid leukemia (AML) cell lines. XPO1, also known as chromosome maintenance protein 1 (CRM1), is an important nuclear-cytoplasmic exporter in eukaryotes that transports a variety of protein cargoes from the nucleus to the cytoplasm, such as tumor suppressor proteins, cell cycle regulators and apoptosis inducers. Inhibition of XPO1-mediated nuclear export is a promising therapeutic strategy for many cancers, including chronic lymphocytic leukemia (CLL), AML, and aggressive lymphomas.

References:

1. Etchin J, Berezovskaya A, Conway AS, et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia, 2017, 31(1): 143-150.

2. Hing ZA, Fung HY, Ranganathan P, et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia, 2016, 30(12): 2364-2372.

试验操作

Cell experiment:[2]
Cell lines	Human primary CLL cells and diffuse large B-cell lymphoma cell lines
Reaction Conditions	0 ~ 10 μM Eltanexor (KPT-8602) for 48 h incubation
Applications	Eltanexor (KPT-8602) induced dose-dependent killing of primary CLL cells when compared to vehicle. Eltanexor (KPT-8602) also caused dose-dependent cytotoxicity in the activated B-cell (ABC) subtype and germinal center (GC) subtype of diffuse large B-cell lymphoma cell lines.
Animal experiment:[1]
Animal models	NOD-SCID-IL2Rcγ^null(NSG) mice intravenously injected with various AML cell lines
Dosage form	15 mg/kg Once daily by oral route for 4 weeks
Applications	In various AML patient-derived xenograft models, Eltanexor (KPT-8602) exhibited superior anti-leukemic activity and better tolerability than Selinexor, with nearly complete elimination of human AML cells in the normal karyotype AML model. Moreover, KPT-8602 was minimally toxic to normal hematopoietic stem and progenitor cells.
Note	The technical data provided above is for reference only.
	References: 1. Etchin J, Berezovskaya A, Conway AS, et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia, 2017, 31(1): 143-150. 2. Hing ZA, Fung HY, Ranganathan P, et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia, 2016, 30(12): 2364-2372.