1. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related Anti-infection
  2. Topoisomerase ADC Payload Antibiotic
  3. Rebeccamycin

Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.

For research use only. We do not sell to patients.

Rebeccamycin

Rebeccamycin Chemical Structure

CAS No. : 93908-02-2

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Description

Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II[1][2].

IC50 & Target[1]

Topoisomerase I

 

Traditional Cytotoxic Agents

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.3 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity in vitro against A549 (human non-small lung carcinoma) cell line.
Antiproliferative activity in vitro against A549 (human non-small lung carcinoma) cell line.
[PMID: 11882002]
B16 IC50
0.48 μM
Compound: 1
Inhibition of murine B16 Melanoma cell proliferation
Inhibition of murine B16 Melanoma cell proliferation
[PMID: 9341921]
B16 IC50
0.48 μM
Compound: 1 (Rebeccamycin)
Antiproliferative activity measured against murine B16 melanoma cells
Antiproliferative activity measured against murine B16 melanoma cells
[PMID: 9572888]
B16 IC50
0.48 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity against B16 mouse melanoma cells
Antiproliferative activity against B16 mouse melanoma cells
[PMID: 8893841]
CEM-SS CC50
1.05 μM
Compound: 1
The cytotoxicity was evaluated in in HIV -I Lai infected CEM-SS cells.
The cytotoxicity was evaluated in in HIV -I Lai infected CEM-SS cells.
[PMID: 10346933]
CEM-SS CC50
1.05 μM
Compound: 1 (Rebeccamycin)
Cytotoxicity against HIV-1 Lai infected CEM-SS cells
Cytotoxicity against HIV-1 Lai infected CEM-SS cells
[PMID: 10052965]
CEM-SS CC50
1.05 μM
Compound: 1 (Rebeccamycin)
Cytotoxic concentration is tested against CEM-SS cells
Cytotoxic concentration is tested against CEM-SS cells
[PMID: 9572888]
CEM-SS IC50
0.52 μM
Compound: 1
Compound was tested for anti-HIV activity in HIV -I Lai infected CEM-SS cells.
Compound was tested for anti-HIV activity in HIV -I Lai infected CEM-SS cells.
[PMID: 10346933]
CEM-SS IC50
0.52 μM
Compound: 1 (Rebeccamycin)
Anti-HIV-1 activity in CEM-SS cells was measured by the quantification of the reverse transcriptase activity, associated with the virus particles released from HIV-1 infected cells in the culture medium.
Anti-HIV-1 activity in CEM-SS cells was measured by the quantification of the reverse transcriptase activity, associated with the virus particles released from HIV-1 infected cells in the culture medium.
[PMID: 10052965]
CEM-SS IC50
0.52 μM
Compound: 1 (Rebeccamycin)
Inhibitory concentration is tested in HIV-1 Lai-infected CEM-SS cells
Inhibitory concentration is tested in HIV-1 Lai-infected CEM-SS cells
[PMID: 9572888]
HT-29 IC50
0.3 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity in vitro against HT-29 (human colon carcinoma) cell line.
Antiproliferative activity in vitro against HT-29 (human colon carcinoma) cell line.
[PMID: 11882002]
HT-29 IC50
0.3 μM
Compound: Rebeccamycin
In vitro antiproliferative activity against human colon carcinoma HT-29 cells
In vitro antiproliferative activity against human colon carcinoma HT-29 cells
[PMID: 15743184]
K562 IC50
0.2 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity in vitro against K-562 (human leukemia) cell line.
Antiproliferative activity in vitro against K-562 (human leukemia) cell line.
[PMID: 11882002]
K562 IC50
4 μM
Compound: Reb
Anticancer activity against human K562 cells
Anticancer activity against human K562 cells
[PMID: 18653350]
K562 IC50
6 μM
Compound: Rebeccamycin
Inhibitory concentration against K5662 leukemia cell line in MTS assay
Inhibitory concentration against K5662 leukemia cell line in MTS assay
[PMID: 15801850]
L1210 IC50
0.1 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity tested in vitro against L1210 (murine leukemia) cell line.
Antiproliferative activity tested in vitro against L1210 (murine leukemia) cell line.
[PMID: 11882002]
L1210 IC50
0.14 μM
Compound: Rebeccamycin
In vitro antiproliferative activity against murine leukemia L1210 cells
In vitro antiproliferative activity against murine leukemia L1210 cells
[PMID: 15743184]
L1210 IC50
0.14 μM
Compound: Rebeccamycin
Cytotoxicity activity against mouse L1210 cells by MTT assay
Cytotoxicity activity against mouse L1210 cells by MTT assay
[PMID: 20566289]
P388 IC50
0.3 μM
Compound: 1 ; Rebeccamycin
Antiproliferative activity against P388 Murine Leukemia cells
Antiproliferative activity against P388 Murine Leukemia cells
[PMID: 8893841]
P388 IC50
0.5 μM
Compound: 1
Inhibition of P388 murine leukemia cell proliferation
Inhibition of P388 murine leukemia cell proliferation
[PMID: 9341921]
P388 IC50
1.22 μM
Compound: 1
In vitro inhibitory concentration against murine P388 leukemia cell proliferation
In vitro inhibitory concentration against murine P388 leukemia cell proliferation
[PMID: 10346933]
P388 IC50
1.22 μM
Compound: 1 (Rebeccamycin)
Cytotoxicity against P388 leukemia cells
Cytotoxicity against P388 leukemia cells
[PMID: 10052965]
P388 IC50
1.22 μM
Compound: 1 (Rebeccamycin)
Antiproliferative activity measured against P388 Leukemia cells
Antiproliferative activity measured against P388 Leukemia cells
[PMID: 9572888]
P388 IC50
10.5 μM
Compound: 1 (Rebeccamycin)
Cytotoxicity against P388/CPT5 leukemia cells.
Cytotoxicity against P388/CPT5 leukemia cells.
[PMID: 10052965]
P388CPT5 IC50
10.5 μM
Compound: 1
In vitro inhibitory concentration against murine P388CPT5 leukemia cell proliferation
In vitro inhibitory concentration against murine P388CPT5 leukemia cell proliferation
[PMID: 10346933]
P388CPT5 IC50
10.5 μM
Compound: 1 (Rebeccamycin)
Antiproliferative activity measured against P388CPT5 cells resistant to Topoisomerase I inhibitor Camptothecin
Antiproliferative activity measured against P388CPT5 cells resistant to Topoisomerase I inhibitor Camptothecin
[PMID: 9572888]
SW-620 IC50
4 μM
Compound: Reb
Anticancer activity against human SW620 cells
Anticancer activity against human SW620 cells
[PMID: 18653350]
SW-620 IC50
4 μM
Compound: Rebeccamycin
Inhibitory concentration against SW620 colorectal carcinoma cell line in MTS assay
Inhibitory concentration against SW620 colorectal carcinoma cell line in MTS assay
[PMID: 15801850]
In Vitro

Rebeccamycin is an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116 (colon carcinoma), and KB (nasopharyngeal carcinoma) [1].
Rebeccamycin shows antibacterial activity against several Gram-positive bacteria, including Staphylococcus aureus and Streptococcus faecalis[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rebeccamycin (2-256 mg/kg; i.p.; daily for 9 days) prolongs survival in B16 melanoma, L1210 leukemia[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CDF1 mice (B16 melanoma, L1210 leukemia)[2]
Dosage: 2, 4, 8, 16, 32, 64, 128, 256 mg/kg
Administration: I.p.; daily for 9 days
Result: Prolongation of survival of the mice at dose levels ranging from 8 to 256 mg/kg.
Molecular Weight

570.38

Formula

C27H21Cl2N3O7

CAS No.
SMILES

O=C(N1)C(C2=C3N([C@@H]([C@@H]([C@@H](O)[C@@H]4OC)O)O[C@@H]4CO)C5=C2C=CC=C5Cl)=C(C(C6=CC=C7)=C3NC6=C7Cl)C1=O

Structure Classification
Initial Source

the mycelium

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
Rebeccamycin
Cat. No.:
HY-19825
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