KPT-185

Modify Date: 2024-01-13 14:56:20

KPT-185 Structure
KPT-185 structure
Common Name KPT-185
CAS Number 1333151-73-7 Molecular Weight 355.312
Density 1.3±0.1 g/cm3 Boiling Point 458.8±55.0 °C at 760 mmHg
Molecular Formula C16H16F3N3O3 Melting Point N/A
MSDS N/A Flash Point 231.3±31.5 °C

 Use of KPT-185


KPT-185 is an orally bioavailable selective inhibitor of CRM1 amd displayes potent antiproliferative properties at submicromolar concentrations (IC50 values:100-500nM), induced apoptosis (average 5-fold increase), cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts.IC50 value: 100-500 nM (AML cell lines) [1]Target: CRM1in vitro: Submicromolar concentrations of KPT-185 inhibited leukemia cell proliferation, with IC50 values ranging from 100nM to 500nM (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1). KPT-185 at the predetermined IC50 value induced cell-cycle arrest at G1 with respect to vehicle-treated-control (DMSO) in MV4-11 (82.2% ± 3.69% vs 71.55% ± 0.21%, P < .01), OCI/AML3 (83.05% ± 6.84% vs 55.1% ± 2.26%, P < .01), and MOLM-13 (82.72% ± 1.14% vs 57.55 ± 3.46%, P < .01) cells at 24 hours. A significant accumulation of p53 in the nucleus of MV4-11 and OCI-AML3 was observed after treatment with KPT-185 [1]. KPT-185 also induced CRM1 accumulation in the nucleus, resulting in CRM1 degradation by the proteasome [2]. in vivo: In melanoma xenograft models, CRM1 inhibition reduces tumor growth independent of BRAF or NRAS status and induces complete regression of BRAF V600E tumors when combined with BRAF inhibition [3].

 Names

Name propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate
Synonym More Synonyms

 KPT-185 Biological Activity

Description KPT-185 is an orally bioavailable selective inhibitor of CRM1 amd displayes potent antiproliferative properties at submicromolar concentrations (IC50 values:100-500nM), induced apoptosis (average 5-fold increase), cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts.IC50 value: 100-500 nM (AML cell lines) [1]Target: CRM1in vitro: Submicromolar concentrations of KPT-185 inhibited leukemia cell proliferation, with IC50 values ranging from 100nM to 500nM (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1). KPT-185 at the predetermined IC50 value induced cell-cycle arrest at G1 with respect to vehicle-treated-control (DMSO) in MV4-11 (82.2% ± 3.69% vs 71.55% ± 0.21%, P < .01), OCI/AML3 (83.05% ± 6.84% vs 55.1% ± 2.26%, P < .01), and MOLM-13 (82.72% ± 1.14% vs 57.55 ± 3.46%, P < .01) cells at 24 hours. A significant accumulation of p53 in the nucleus of MV4-11 and OCI-AML3 was observed after treatment with KPT-185 [1]. KPT-185 also induced CRM1 accumulation in the nucleus, resulting in CRM1 degradation by the proteasome [2]. in vivo: In melanoma xenograft models, CRM1 inhibition reduces tumor growth independent of BRAF or NRAS status and induces complete regression of BRAF V600E tumors when combined with BRAF inhibition [3].
Related Catalog
References

[1]. Ranganathan P, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120(9):1765-73.

[2]. Zhang K, et al. Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma. Exp Hematol. 2013 Jan;41(1):67-78.e4.

[3]. Salas Fragomeni RA, et al. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12(7):1171-9.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 458.8±55.0 °C at 760 mmHg
Molecular Formula C16H16F3N3O3
Molecular Weight 355.312
Flash Point 231.3±31.5 °C
Exact Mass 355.114380
PSA 66.24000
LogP 4.24
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.526
Storage condition -20°C

 Safety Information

Hazard Codes Xi

 Synonyms

2-Propenoic acid, 3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 1-methylethyl ester, (2Z)-
Isopropyl (2Z)-3-{3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}acrylate
(Z)-isopropyl 3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate
S7125
KPT-185
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: KPT-185
  • Price: $350.0/100mg $700.0/250mg $1300.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: ¥798/10 mM * 1 mL in DMSO

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