Chemical Structure : DEPTOR-IN-2
CAS No.:
2138479-15-7
DEPTOR-IN-2
(Compound 3g, Drug 3g)
Catalog No.: PC-27311Not For Human Use, Lab Use Only.
DEPTOR-IN-2 (Compound 3g, Drug 3g) is a small molecule inhibitor of DEPTOR-mTOR interaction, prevents binding of recombinant DEPTOR to mTOR with IC50 of 1 uM, induces DEPTOR degradation, shows anti-myeloma cytotoxic properties.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DEPTOR-IN-2 (Compound 3g, Drug 3g) is a small molecule inhibitor of DEPTOR-mTOR interaction, prevents binding of recombinant DEPTOR to mTOR with IC50 of 1 uM, induces DEPTOR degradation, shows anti-myeloma cytotoxic properties.
DEPTOR-IN-2 (Compound 3g, Drug 3g) inhibits 8226 cells in MTT assays with IC50 of 0.12 uM.
DEPTOR-IN-2 (Compound 3g, Drug 3g) (0.5 uM) prevents DEPTOR-mTOR binding in MM cells.
DEPTOR-IN-2 (Compound 3g, Drug 3g) decreases phosphorylation of AKT (T308) in 8226 and OPM-2 MM cells.
DEPTOR-IN-2 (Compound 3g, Drug 3g) induces p70 phosphorylation.
DEPTOR-IN-2 (Compound 3g, Drug 3g) (5 and 10 mg/kg, daily IP injection) demonstrates slowing tumor growth and prolonging survival in xenograft tumors.
Physicochemical Properties
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M.Wt
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375.98
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Formula
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C12H5Cl4F3N2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(Perchlorocyclopenta-2,4-dien-1-ylidene)-2-(3-(trifluoromethyl)phenyl)hydrazine
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References
1. Jihye Lee, et al. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4714-4724.
2. Vega MI, et al. Mol Cancer Ther. 2019 Oct;18(10):1822-1831.
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