2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. YCH1899

YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.

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YCH1899 Chemical Structure

YCH1899 Chemical Structure

CAS No. : 3032451-66-1

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YCH1899 Related Antibodies

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Description

YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats[1].

IC50 & Target

PARP-1

<0.001 nM (IC50)

PARP-2

<0.001 nM (IC50)

PARP3

1.1 nM (IC50)

PARP4

1.0 nM (IC50)

TNKS1

3.8 nM (EC50)

TNKS2

12.4 nM (IC50)

PARA6

9.5 nM (IC50)

PARP-7

7.3 nM (IC50)

ARTD10/PARP10

10.8 nM (IC50)

PARA11

2.166 μM (IC50)

human PARP12

14.1 nM (IC50)

PARP14

35.914 μM (IC50)

PARP15

51.623 nM (IC50)

In Vitro

YCH1899 (7 days) shows obvious anti-proliferation activity on Capan-1, Capan-1/OP and Capan-1/TP cells, with IC50 of 0.10, 0.89 and 1.13 nM, respectively.[1].
YCH1899 (0.001-1 μM, 4 h) stabilizes PARP1-DNA complexes and suppresses PARP formation[1].
YCH1899 (3.5 h) inhibits the proliferation of BRCA mutant/wild-type cells (V-C8, V79, HCT-15, HCC1937) with IC50s ranging from 1.19-44.24 nM[1].
YCH1899 (1 μM, 24 h) causes a large increase in the number of γH2AX foci in Capan-1、Capan-1/OP、Capan-1/TP cells[1].
YCH1899 (1 μM, 48 h) induces a dramatic decrease in HR (Homologous Recombination) repair activity in U2OS-DR-GFP cells[1].

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

YCH1899 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCC1937, HCT-15, MDA-MB-436, UWB1.289, UWB1.289+BRCA1, V–C8, V79 cells
Concentration: 0-1 μM approximately
Incubation Time: 24 h
Result: Inhibited the proliferation of BRCA-Deficient/Wild-Type Cells and IC50s value were 4.54, 44.24, 0.52, 0.02, 0.34, 1.19, 29.32nM, respectively.

Immunofluorescence[1]

Cell Line: Capan-1, Capan-1/OP cells, Capan-1/TP cells
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 24 h
Result: Increased γH2AX level in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Capan-1 and Capan-1/OP cells
Concentration: 1, 10, 100 nM
Incubation Time: 4 h
Result: Improved stability of PARP1-DNA complexes and induced chromatin-bound PARP1 accumulation in the presence of MMS (methanesulfonate).
Inhibited PARP formation in the presence of 0.1% H2O2.
In Vivo

YCH1899 (5 mg/kg, intravenous injection ) has a moderate clearance rate in rats[1].
YCH1899 overcomes acquired Talazoparib resistance and has a significant regression of tumor volume in MDA-MB-436/OP (6.25, 12.5, and 25 mg/kg, orally, once a day for 27 days) and Capan-1/R-in vivo xenografts (12.5 and 25 mg/kg, orally, once a day for 21 days ) [1].

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

Animal Model: MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice[1]
Dosage: 12.5 and 25 mg/kg
Administration: Oral administration
Result: Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kg
Inhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.
Animal Model: rats[1]
Dosage: 5 mg/kg
Administration: Intravenous injection
Result: Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
Molecular Weight

549.35

Formula

C25H18BrFN6O3
CAS No.
SMILES

O=C1NN=C(C2=CC=CC=C21)CC3=CC=C(C(C(N4CCN5C(C4)=NN=C5C6=CC=C(O6)Br)=O)=C3)F
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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YCH1899 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:

YCH18993032451-66-1YCH 1899YCH-1899PARPpoly ADP ribose polymeraseHCC1937UWB1.289PARPiCapan-1 cellMDA-MB-436/OP cellsxenograft mouse tumor modelsInhibitorinhibitorinhibit

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