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.

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

YCH1899 Chemical Structure

YCH1899 Chemical Structure

CAS No. : 3032451-66-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
5 mg USD 200 In-stock
10 mg USD 325 In-stock
25 mg USD 650 In-stock
50 mg USD 1050 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

YCH1899 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 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.

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.
Appearance

Solid

Color

White to off-white

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (36.41 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8203 mL 9.1017 mL 18.2033 mL
5 mM 0.3641 mL 1.8203 mL 3.6407 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (3.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (3.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8203 mL 9.1017 mL 18.2033 mL 45.5083 mL
5 mM 0.3641 mL 1.8203 mL 3.6407 mL 9.1017 mL
10 mM 0.1820 mL 0.9102 mL 1.8203 mL 4.5508 mL
15 mM 0.1214 mL 0.6068 mL 1.2136 mL 3.0339 mL
20 mM 0.0910 mL 0.4551 mL 0.9102 mL 2.2754 mL
25 mM 0.0728 mL 0.3641 mL 0.7281 mL 1.8203 mL
30 mM 0.0607 mL 0.3034 mL 0.6068 mL 1.5169 mL
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YCH1899 Related Classifications

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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