1333151-73-7
1333151-73-7 structure
- Name: KPT-185
- Chemical Name: propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate
- CAS Number: 1333151-73-7
- Molecular Formula: C16H16F3N3O3
- Molecular Weight: 355.312
- Catalog: Biochemical Inhibitor Transmembrane Transporters CRM1 inhibitor
- Create Date: 2017-04-11 22:06:04
- Modify Date: 2024-01-13 14:56:20
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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].
| Name | propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate |
|---|---|
| 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 |
| 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]. |
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| Density | 1.3±0.1 g/cm3 |
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| 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 |
| Hazard Codes | Xi |
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