DD-CIP2
DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research.
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- Formule: C52H54ClFN10O5S
- Masse moléculaire:985.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
DD-CIP2 can target a broad spectrum of cancers with IC50 = 12 nM in Jurkat cell, IC50 = 12 nM in KARPASS422 cell, IC50 = 11 nM in Raji cell, IC50 = 2 nM in Daudi cell, IC50 = 9.3 nM in TYK-nu cell, and IC50 < 10 nM in MDA-MB-436, IC50 = 0.8 nM in SU-DHL-5 cells, IC50 = 4.6 nM in MOLT-4[1].
[1]
DD-CIP2 displays only a modest increase of PARP1 occupancy with EC50 = 42 nM[1].
DD-CIP2 (0.1-100 nM, 24 h) induces PARP1-BRD4 interaction in HEK293T cells and reduces DNA damage in both GLC16 and NCI-H82 cell lines[1].
DD-CIP2 (0.1-0.8 nM, 72 h) demonstrates the dependency on the PARP-170 BRD4 association in SU-DHL-5 cell[1].
DD-CIP2 (10 μM, 24 h) stalles cell cycle progression in GLC16 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:0.1, 1, 10 and 100 nM
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Incubation Time:24 h
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Result:Elevated levels of γH2AX and cleaved PARP1 in both GLC16 and NCI-H82 cell.
Increased the phosphorylation of RPA32 at Ser4/Ser8 in both GLC16 and NCI-H82 cell.
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Cell Line:GLC16 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Provoked a dose-dependent accumulation of 199 cells in the G2/M phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GLC16 cells (2 × 106, s.c.) induced NU-Foxn1nu mice (8 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p., once for 5 days
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Result:Induced a dose-dependent increase in γH2AX and cleaved PARP1, confirming target engagement.
Was well tolerated at doses up to 20 mg/kg, with no significant body weight loss.
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Animal Model:GLC16 cells (2 × 106, s.c.) induced NU-Foxn1nu mice (8 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p., once for 28 days
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Result:Showed strong tumor regression as early as day 3, with 210 durable suppression maintained throughout the experiment period.
Detected no obvious toxicity as indicated by steady body weight.
Chemical Information
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Masse moléculaire 985.57
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Formule C52H54ClFN10O5S
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SMILES
FC1=CC=C(CC2=NNC(C3=CC=CC=C32)=O)C=C1C(N(CC4)CCN4C(C(CC5)CCC65CCN(C(CNC(C[C@H]7C8=NN=C(C)N8C(SC(C)=C9C)=C9C(C%10=CC=C(Cl)C=C%10)=N7)=O)=O)CC6)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DD-CIP2 Related Classifications
HY-179585 Related Classifications
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