Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H27N5O3 |
Molecular Weight | 397.4708 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CO[C@H]1CC[C@@H](CC1)N2C(=O)CNC3=C2N=C(C=N3)C4=CN=C(C=C4)C(C)(C)O
InChI
InChIKey=UFKLYTOEMRFKAD-SHTZXODSSA-N
InChI=1S/C21H27N5O3/c1-21(2,28)17-9-4-13(10-22-17)16-11-23-19-20(25-16)26(18(27)12-24-19)14-5-7-15(29-3)8-6-14/h4,9-11,14-15,28H,5-8,12H2,1-3H3,(H,23,24)/t14-,15-
CC-223 is an orally available inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. CC-223 disrupted mitochondrial function, and induced mitochondrial permeability transition pore (mPTP) opening and reactive oxygen species (ROS) production. CC-223 is currently in phase II clinical trials for the treatment of Multiple myeloma; Non-Hodgkin's lymphoma; Solid tumours. The most common treatment-related adverse events were hyperglycemia, fatigue and rash.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2842 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25855786 |
16.0 nM [IC50] | ||
Target ID: CHEMBL4005 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25855786 |
4.0 µM [IC50] | ||
Target ID: CHEMBL3142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25855786 |
0.84 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02031419
20 mg or 30 mg once daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25855786
CC-223 showed a concentration-dependent reduction in each marker, with IC50 values of 31 nmol/L for pS6RP, 405 47 nmol/L for p4EBP1, and 11 10 nmol/L for pAKT(S473). CC-223 inhibited both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers across the panel with IC50 ranges of 27 to 184 nmol/L for pS6RP, 120 to 1,050 nmol/L for p4EBP1 and 11 to 150 nmol/L for pAKT
(S473).
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FDA ORPHAN DRUG |
407913
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DB12570
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CHEMBL3545151
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GH-13
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C92575
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1228013-30-6
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I8RA3543SY
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ACTIVE MOIETY