2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. XR5944

XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer.

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XR5944

XR5944 Chemical Structure

CAS No. : 343247-32-5

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Based on 1 publication(s) in Google Scholar

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Description

XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer[1].

Cellular Effect
Cell Line Type Value Description References
CAKI-1 GI50
< 10 nM
Compound: 8
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the CAK1 human cell line
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the CAK1 human cell line
[PMID: 11311063]
D3F IC50
4.4 nM
Compound: 8
Concentration of the drug to reduce cell number to 50% of controls in D3F cell line
Concentration of the drug to reduce cell number to 50% of controls in D3F cell line
[PMID: 11311063]
HCT-116 GI50
< 10 nM
Compound: 8
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the HTC116 human cell line
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the HTC116 human cell line
[PMID: 11311063]
HT-29 GI50
< 10 nM
Compound: 8
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the HT-29 human cell line
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the HT-29 human cell line
[PMID: 11311063]
HT-29 IC50
0.08 nM
Compound: 8
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in HT-29 (human colon)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in HT-29 (human colon)
[PMID: 11311063]
MCF7 GI50
< 10 nM
Compound: 8
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the MCF-7 human cell line
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the MCF-7 human cell line
[PMID: 11311063]
MOLT-4 IC50
0.0062 nM
Compound: 8
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in MOLT-4 (human leukemia)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in MOLT-4 (human leukemia)
[PMID: 11311063]
P388 IC50
21 nM
Compound: 8
Inhibitory concentration required to reduce cell number to 50% of control cultures in P388 (murine leukemia cell line)
Inhibitory concentration required to reduce cell number to 50% of control cultures in P388 (murine leukemia cell line)
[PMID: 11311063]
SK-OV-3 GI50
< 10 nM
Compound: 8
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the SKOV3 human cell line
Inhibitory concentration required to reduce cell growth to 50% of control cultures in the SKOV3 human cell line
[PMID: 11311063]
U-937 IC50
0.047 nM
Compound: 8
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in U937 (human leukemia)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in U937 (human leukemia)
[PMID: 11311063]
Molecular Weight

586.69

Formula

C34H34N8O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC2=NC3=CC=CC(C)=C3N=C21)NCCNCCNCCNC(C4=CC=CC5=NC6=CC=CC(C)=C6N=C54)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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XR5944 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XR5944343247-32-5XR 5944XR-5944Endogenous MetaboliteInhibitorinhibitorinhibit

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