Stereochemistry | ABSOLUTE |
Molecular Formula | C17H15F2IN4O4 |
Molecular Weight | 504.2267 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C(F)=C(NC2=CC=C(I)C=C2F)C3=C1N=CN(C[C@@H](O)CO)C3=O
InChI
InChIKey=RCLQNICOARASSR-SECBINFHSA-N
InChI=1S/C17H15F2IN4O4/c1-23-15-12(16(27)24(7-21-15)5-9(26)6-25)14(13(19)17(23)28)22-11-3-2-8(20)4-10(11)18/h2-4,7,9,22,25-26H,5-6H2,1H3/t9-/m1/s1
Molecular Formula | C17H15F2IN4O4 |
Molecular Weight | 504.2267 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
TAK-733 had been developed by Millennium Pharmaceuticals (subsidiary of Takeda) for the treatment of adult patients with advanced non-hematological malignancies. In 2015, Takeda discontinued this studies. TAK-733 is an inhibitor of MEK that exhibits anticancer chemotherapeutic activity. In tumor explant models, TAK-733 induces tumor regression. In colorectal cancer cells and melanoma cells, this compound suppresses cell growth. Additionally, TAK-733 decreases tumor growth and weight in animal models of lung cancer and melanoma.
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
Patients received oral TAK-733 once daily on days 1-21 in 28-day treatment cycles. Fifty one patients received TAK-733 at one of eleven dose levels: 0.2 mg (n = 1); 0.4 mg (n = 1); 0.8 mg (n = 2);
1.6 mg (n = 2); 3.2 mg (n = 4); 4.4 mg (n = 4); 6 mg
(n = 4); 8.4 mg (n = 9); 11.8 mg (n = 8); 16 mg (n = 9); and
22 mg (n = 7)
Route of Administration:
Oral