1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. CH-0793076

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (CH-0793076 TFA) usually boasts enhanced water solubility and stability.

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

CH-0793076 Chemical Structure

CH-0793076 Chemical Structure

CAS No. : 534605-78-2

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Description

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].

IC50 & Target[1]

Topoisomerase I

2.3 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.36 nM
Compound: 7c
Antiproliferative activity against human HCT116 cells after 3 days
Antiproliferative activity against human HCT116 cells after 3 days
[PMID: 19254843]
NCI-H460 IC50
2.3 nM
Compound: 7c
Antiproliferative activity against human NCI-H460 cells after 3 days
Antiproliferative activity against human NCI-H460 cells after 3 days
[PMID: 19254843]
PC-6 IC50
0.18 nM
Compound: 7c
Antiproliferative activity against human PC6 cells carrying pRC after 6 days
Antiproliferative activity against human PC6 cells carrying pRC after 6 days
[PMID: 19254843]
PC-6 IC50
0.35 nM
Compound: 7c
Antiproliferative activity against human PC6 expressing BCRP cells after 6 days
Antiproliferative activity against human PC6 expressing BCRP cells after 6 days
[PMID: 19254843]
QG-56 IC50
2.3 nM
Compound: 7c
Antiproliferative activity against human QG56 cells after 3 days
Antiproliferative activity against human QG56 cells after 3 days
[PMID: 19254843]
In Vitro

CH0793076 (TP3076) (6 days at 37°C) shows antiproliferative activity against PC-6/BCRP and PC-6/pRC cells, with IC50s of 0.35 and 0.18 nM, respectively[1].

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

In Vivo

TP300 (1-100 mg/kg; bolus intravenous injection once per week for 3 weeks, for a total of three doses), a water-soluble prodrug of CH0793076, shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP (WiDr, HT-29, NCI-H460 and AsPC-1, HCT116, COLO 201, HCT-15, Calu-6 and NCI-N87)[1].

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

Molecular Weight

458.51

Formula

C26H26N4O4

CAS No.
SMILES

O=C1[C@](O)(CC)C(C=C23)=C(CO1)C(N2CC(C3=N4)=C5N(CCCCC)C=NC6=C5C4=CC=C6)=O

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:
CH-0793076
Cat. No.:
HY-107096
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