KRX-0601
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 203060

CAS#: 112953-11-4

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).

Chemical Structure

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KRX-0601
CAS# 112953-11-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 203060
Name: KRX-0601
CAS#: 112953-11-4
Chemical Formula: C28H26N4O4
Exact Mass: 482.20
Molecular Weight: 482.540
Elemental Analysis: C, 69.70; H, 5.43; N, 11.61; O, 13.26

Price and Availability

Size Price Availability Quantity
1mg USD 450 2 Weeks
5mg USD 1350 2 Weeks
Bulk inquiry

Synonym: UCN01, UCN-01, UCN 01, Staurosporine 7hydroxystaurosporine, KW2401, KW-2401, KW 2401

IUPAC/Chemical Name: (5R,7R,8R,9S,14S)-14-hydroxy-8-methoxy-9-methyl-7-(methylamino)-6,7,8,9,14,15-hexahydro-5H,16H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-16-one

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

Appearance: Solid powder

Purity: 97%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:      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.      

Product Data:
Product Data
Certificate of Analysis:
View CoA: current batch, Lot#S20G11M13
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: A nonspecific protein kinase inhibitor.
In vitro activity: UCN-01 induced cell cycle arrest and apoptosis in the human osteosarcoma, U2-OS cells. In addition, the migration ability was also reduced, suggesting UCN-01 inhibited cell growth and migration. Reference: J Cell Biochem. 2018 Jun;119(6):4729-4741. https://pubmed.ncbi.nlm.nih.gov/29280173/
In vivo activity: UCN-01 causes significant, reversible arrest of normal gut epithelial cells at 24 h; this arrest persists for up to 7 days. Normal cellular proliferation returns by 2 weeks. Pre-treatment of both non-tumour-bearing and MDA-MB-468 tumour-bearing mice with UCN-01 prior to bolus 5-FU (450 mg/kg) yielded enhanced therapeutic efficacy with significantly decreased tumour volumes and increased survival. Reference: Br J Cancer. 2020 Mar;122(6):812-822. https://pubmed.ncbi.nlm.nih.gov/31942030/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Ethanol 1.0 2.07

Preparing Stock Solutions

The following data is based on the product molecular weight 482.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lien WC, Chen TY, Sheu SY, Lin TC, Kang FC, Yu CH, Kuan TS, Huang BM, Wang CY. 7-hydroxy-staurosporine, UCN-01, induces DNA damage response, and autophagy in human osteosarcoma U2-OS cells. J Cell Biochem. 2018 Jun;119(6):4729-4741. doi: 10.1002/jcb.26652. Epub 2018 Feb 28. PMID: 29280173. 2. Alcántara-Hernández R, Hernández-Méndez A, García-Sáinz JA. The phosphoinositide-dependent protein kinase 1 inhibitor, UCN-01, induces fragmentation: possible role of metalloproteinases. Eur J Pharmacol. 2014 Oct 5;740:88-96. doi: 10.1016/j.ejphar.2014.06.057. Epub 2014 Jul 10. PMID: 25016091.
In vitro protocol: 1. Lien WC, Chen TY, Sheu SY, Lin TC, Kang FC, Yu CH, Kuan TS, Huang BM, Wang CY. 7-hydroxy-staurosporine, UCN-01, induces DNA damage response, and autophagy in human osteosarcoma U2-OS cells. J Cell Biochem. 2018 Jun;119(6):4729-4741. doi: 10.1002/jcb.26652. Epub 2018 Feb 28. PMID: 29280173. 2. Alcántara-Hernández R, Hernández-Méndez A, García-Sáinz JA. The phosphoinositide-dependent protein kinase 1 inhibitor, UCN-01, induces fragmentation: possible role of metalloproteinases. Eur J Pharmacol. 2014 Oct 5;740:88-96. doi: 10.1016/j.ejphar.2014.06.057. Epub 2014 Jul 10. PMID: 25016091.
In vivo protocol: 1. Mull BB, Livingston JA, Patel N, Bui T, Hunt KK, Keyomarsi K. Specific, reversible G1 arrest by UCN-01 in vivo provides cytostatic protection of normal cells against cytotoxic chemotherapy in breast cancer. Br J Cancer. 2020 Mar;122(6):812-822. doi: 10.1038/s41416-019-0707-z. Epub 2020 Jan 16. PMID: 31942030; PMCID: PMC7078276. 2. Dudgeon C, Wang P, Sun X, Peng R, Sun Q, Yu J, Zhang L. PUMA induction by FoxO3a mediates the anticancer activities of the broad-range kinase inhibitor UCN-01. Mol Cancer Ther. 2010 Nov;9(11):2893-902. doi: 10.1158/1535-7163.MCT-10-0635. Epub 2010 Oct 26. PMID: 20978166; PMCID: PMC2978764.

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