Eltanexor (KPT-8602)

Catalog No.

B8335

A second-generation, orally bioavailable XPO1/CRM1 inhibitor

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Grouped product items
Size	Price	Stock
1mg	$72.00	In stock
5mg	$216.00	In stock
10mg	$315.00	In stock
50mg	$855.00	In stock

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Background
Chemical Properties
Protocol
Quality Control

Background

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.

Chemical Properties

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
SDF	Download SDF
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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

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-IL2Rcγnull (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.

Quality Control

Quality Control & MSDS

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Purity = 99.80%

Chemical structure

Eltanexor (KPT-8602)

mRNA synthesis

Tyramide Signal Amplification (TSA)

Phos Binding Reagent Acrylamide

Cell Counting Kit-8 (CCK-8)

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