WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 203060
Description: KRX-0601, also known as UCN-01, is a synthetic derivative of staurosporine with antineoplastic activity. 7-hydroxystaurosporine inhibits many phosphokinases, including the serine/threonine kinase AKT, calcium-dependent protein kinase C, and cyclin-dependent kinases. This agent arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
MedKoo Cat#: 203060
Chemical Formula: C28H26N4O4
Exact Mass: 482.19541
Molecular Weight: 482.53
Elemental Analysis: C, 69.70; H, 5.43; N, 11.61; O, 13.26
Synonym: UCN01, UCN-01, UCN 01, Staurosporine 7hydroxystaurosporine, KW2401, KW-2401, KW 2401
IUPAC/Chemical Name: 9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3R,9S,10R,11R,13R)-
InChi Key: GUAIZLSIUMRUNL-IHQXTNFTSA-N
InChi Code: InChI=1S/C28H27N4O4/c1-28-7-4-8-31-19-9-14(33)10-21(34)24(19)23-18-13-30-12-17(18)22-16-6-5-15(36-28)11-20(16)32(29-2,27(28)35-3)26(22)25(23)31/h4-7,9,12-15,27,29,33H,8,10-11H2,1-3H3/b7-4-/t14-,15-,27+,28-/m0/s1
SMILES Code: O=C(C[C@@H](O)C=C12)C1=C3C4=CN=CC4=C5C6=C3N2C/C=C\[C@@](O7)(C)[C@@H](OC)[N@@]6(NC)C8=C5C=C[C@@]7([H])C8
KRX-0601 is a novel multi-kinase inhibitor for the treatment of cancer which, in pre-clinical models, has demonstrated a synergistic effect with agents inhibiting the PI3K pathway, including KRX-0401. KRX-0601 is currently in several Phase II clinical trials both as a single agent and in combination with other anticancer agents which are being conducted under the direction and sponsorship of the National Cancer Institute. KRX-0601 is an anticancer drug that belongs to the family of drugs called staurosporine analogs which have demonstrated an ability to inhibit multiple kinases involved in cell-cycle progression and apoptosis, including Chk-1 and PDK1. In pre-clinical studies, KRX-0601 has demonstrated synergistic effect with DNA-damaging agents including chemotherapy and radiation therapy. In-vitro, KRX-0601 has been shown to be synergistic with agents affecting the PI3-K pathway including KRX-0401 and mTOR inhibitors. In clinical trials, as reported by investigators at the National Cancer Institute, durable single-agent responses have been seen in patients with anaplastic large-cell lymphoma. We expect to continue exploring the potential utility of KRX-0601 over the next year.