1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. 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.

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

YCH1899 Chemical Structure

YCH1899 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

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

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

YCH1899 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
YCH1899
Cat. No.:
HY-155993
Quantity:
MCE Japan Authorized Agent: