Back to products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents in preclinical trials
Anticancer molecular libraries
Other drug agents
Bio-reagents and biochemicals
MedKoo product information:
Description of KRX-0601:
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
Current developer: Kyowa
Pharmaceutical, Inc. .
MedKoo Code#: 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
Availability and price:
This agent is not in stock, which may be available through custom synthesis.
To inquire quotation and lead time or to ask questions, please send email to
firstname.lastname@example.org to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
Product will be shipped with
supporting analytical data.
Information about this agent
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.
1: Ullal AJ, Pisetsky DS. The release of
microparticles by Jurkat leukemia T cells treated with staurosporine and
related kinase inhibitors to induce apoptosis. Apoptosis. 2010
May;15(5):586-96. PubMed PMID: 20146001.
2: Jiang Z, Jin S, Yalowich JC, Brown KD, Rajasekaran B. The mismatch
repair system modulates curcumin sensitivity through induction of DNA
strand breaks and activation of G2-M checkpoint. Mol Cancer Ther. 2010
Mar;9(3):558-68. Epub 2010 Feb 9. PubMed PMID: 20145018; PubMed Central
3: Despras E, Daboussi F, Hyrien O, Marheineke K, Kannouche PL. ATR/Chk1
pathway is essential for resumption of DNA synthesis and cell survival
in UV-irradiated XP variant cells. Hum Mol Genet. 2010 May
1;19(9):1690-701. Epub 2010 Feb 1. PubMed PMID: 20123862.
4: Thompson AF, Levin LA. Neuronal differentiation by analogs of
staurosporine. Neurochem Int. 2010 Mar;56(4):554-60. Epub 2010 Jan 4.
PubMed PMID: 20043966; PubMed Central PMCID: PMC2831141.
5: Varmark H, Kwak S, Theurkauf WE. A role for Chk2 in DNA damage
induced mitotic delays in human colorectal cancer cells. Cell Cycle.
2010 Jan 15;9(2):312-20. Epub 2010 Jan 23. PubMed PMID: 20023427.
6: Bork U, Lee WK, Kuchler A, Dittmar T, Thévenod F. Cadmium-induced DNA
damage triggers G(2)/M arrest via chk1/2 and cdc2 in p53-deficient
kidney proximal tubule cells. Am J Physiol Renal Physiol. 2010
Feb;298(2):F255-65. Epub 2009 Nov 18. PubMed PMID: 19923412.
7: Kummar S, Gutierrez ME, Gardner ER, Figg WD, Melillo G, Dancey J,
Sausville EA, Conley BA, Murgo AJ, Doroshow JH. A phase I trial of
UCN-01 and prednisone in patients with refractory solid tumors and
lymphomas. Cancer Chemother Pharmacol. 2010 Jan;65(2):383-9. Epub 2009
Nov 6. PubMed PMID: 19894051; PubMed Central PMCID: PMC2854012.
8: Khan N, Mupparaju SP, Hou H, Lariviere JP, Demidenko E, Swartz HM,
Eastman A. Radiotherapy in conjunction with 7-hydroxystaurosporine: a
multimodal approach with tumor pO2 as a potential marker of therapeutic
response. Radiat Res. 2009 Nov;172(5):592-7. PubMed PMID: 19883227;
PubMed Central PMCID: PMC2785035.
9: Cavelier C, Didier C, Prade N, Mansat-De Mas V, Manenti S, Recher C,
Demur C, Ducommun B. Constitutive activation of the DNA damage signaling
pathway in acute myeloid leukemia with complex karyotype: potential
importance for checkpoint targeting therapy. Cancer Res. 2009 Nov
15;69(22):8652-61. Epub 2009 Oct 20. PubMed PMID: 19843865.
10: Kondoh E, Mori S, Yamaguchi K, Baba T, Matsumura N, Cory Barnett J,
Whitaker RS, Konishi I, Fujii S, Berchuck A, Murphy SK. Targeting
slow-proliferating ovarian cancer cells. Int J Cancer. 2010 May
15;126(10):2448-56. PubMed PMID: 19795452.
11: Chen S, Maya-Mendoza A, Zeng K, Tang CW, Sims PF, Loric J, Jackson
DA. Interaction with checkpoint kinase 1 modulates the recruitment of
nucleophosmin to chromatin. J Proteome Res. 2009 Oct;8(10):4693-704.
PubMed PMID: 19694479.
12: Kuntz K, O'Connell MJ. The G(2) DNA damage checkpoint: could this
ancient regulator be the Achilles heel of cancer? Cancer Biol Ther. 2009
Aug;8(15):1433-9. Epub 2009 Aug 22. Review. PubMed PMID: 19574738.
13: Lapenna S, Giordano A. Cell cycle kinases as therapeutic targets for
cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. Review. PubMed PMID:
14: Barakat KH, Torin Huzil J, Luchko T, Jordheim L, Dumontet C,
Tuszynski J. Characterization of an inhibitory dynamic pharmacophore for
the ERCC1-XPA interaction using a combined molecular dynamics and
virtual screening approach. J Mol Graph Model. 2009 Sep;28(2):113-30.
Epub 2009 May 4. PubMed PMID: 19473860.
15: Kumari D, Somma V, Nakamura AJ, Bonner WM, D'Ambrosio E, Usdin K.
The role of DNA damage response pathways in chromosome fragility in
Fragile X syndrome. Nucleic Acids Res. 2009 Jul;37(13):4385-92. Epub
2009 May 21. PubMed PMID: 19465392; PubMed Central PMCID: PMC2715245.
16: Chen CC, Kennedy RD, Sidi S, Look AT, D'Andrea A. CHK1 inhibition as
a strategy for targeting Fanconi Anemia (FA) DNA repair pathway
deficient tumors. Mol Cancer. 2009 Apr 16;8:24. PubMed PMID: 19371427;
PubMed Central PMCID: PMC2672921.
17: Wang X, Lui VC, Poon RT, Lu P, Poon RY. DNA damage mediated s and
g(2) checkpoints in human embryonal carcinoma cells. Stem Cells. 2009
Mar;27(3):568-76. PubMed PMID: 19259937; PubMed Central PMCID:
(Keyword; CAS#; MedKoo code#)