KPT-185
- CAS NO.:1333151-73-7
- Empirical Formula: C16H16F3N3O3
- Molecular Weight: 355.31
- MDL number: MFCD25976761
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:06
What is KPT-185?
The Uses of KPT-185
KPT185 acts as a novel CRM1 inhibitor used in the treatment of acute myeloid leukemia.
Biological Activity
kpt-185 is a selective and irreversible inhibitor of chromosome maintenance protein 1 (crm1) with ic50 values of 100-500nm [1].crm1 is an important nuclear protein export receptor. blocking crm1-mediated nuclear export can result in the suppression of tumors. as an inhibitor of crm1, kpt-185 binds crm1within the cys528 site and prevents crm1from interacting with tumor-suppressor proteins. in the in vitro studies on aml cell lines, kpt-185 inhibits proliferation of a variety of leukemia cells with ic50 values ranging from 100nm to 500nm. it induces cell-cycle arrest at g1 and induces apoptosis. kpt-185 also strongly affects cell colony formation. in addition, the inhibition of crm1 caused by kpt-185 induces differentiation of aml blast. besides that, kpt-185 is also found to inhibit proliferation and induce apoptosis of pancreatic cancer cells including colo-357, hpac and bxpc-3 [1, 2].
References
[1] ranganathan p, yu x, na c, et al. preclinical activity of a novel crm1 inhibitor in acute myeloid leukemia. blood, 2012, 120(9): 1765-1773.
[2] azmi a s, aboukameel a, bao b, et al. selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice. gastroenterology, 2013, 144(2): 447-456.
Properties of KPT-185
Boiling point: | 458.8±55.0 °C(Predicted) |
Density | 1.29±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | insoluble in H2O; ≥17.77 mg/mL in DMSO; ≥25.2 mg/mL in EtOH |
form | solid |
pka | 0.47±0.50(Predicted) |
color | White to off-white |
Safety information for KPT-185
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for KPT-185
New Products
(R)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate Tubulysin M 2,2-diethoxyethanethioamide Tubulysin B 2,2-Difluoropropylamine hydrochloride 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) 1,2,3,6-TETRAHYDROPYRIDINE HYDROCHLORIDE 3-Aminocyclobutanone hydrochloride 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE 3-N-BOC-(S)-AMINO BUTYRONITRILE 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Imeglimin Hydrochloride IH 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 2-(2-Formylphenoxy) acetic acid 2-(2,3-Dihydro- benzofuran-5-yl)-1- morpholin-4-yl- ethanethione Latanoprostene Bunod Lubiprostone Magnesium Trisilicate Flame Retardant Zinc Borate 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carbonitrileRelated products of tetrahydrofuran
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