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KPT 330

Names

[ CAS No. ]:
1393477-72-9

[ Name ]:
KPT 330

[Synonym ]:
UNII-31TZ62FO8F
2-Propenoic acid,3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-,2-(2-pyrazinyl)hydrazide,(2Z)
2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)-
(2Z)-3-{3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-N'-(2-pyrazinyl)acrylohydrazide
selinexor
(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide
KPT-330
Selinexor (KPT-330)

Biological Activity

[Description]:

KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.IC50 value: Target: CRM1in 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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CRM1
Research Areas >> Cancer

[References]

[1]. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27.

[2]. Tai YT, et al. CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications. Leukemia. 2014 Jan;28(1):155-65.


[Related Small Molecules]

KPT-8602 | KPT-185 | KPT-276 | Verdinexor

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C17H11F6N7O

[ Molecular Weight ]:
443.306

[ Exact Mass ]:
443.092926

[ PSA ]:
97.62000

[ LogP ]:
3.62

[ Index of Refraction ]:
1.594

[ Storage condition ]:
-20℃

Precursor & DownStream

Precursor

DownStream

Related Compounds