Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
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)
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ln Vitro |
On Capan-1, Capan-1/OP, and Capan-1/TP cells, YCH1899 (7 days) exhibits strong anti-proliferative action with IC50 values of 0.10, 0.89, and 1.13 nM, respectively [1]. YCH1899 (0.001-1 nM, 4 h) suppresses PARP production while stabilizing the PARP1-DNA complex [1]. The growth of BRCA mutant/wild-type cells (V-C8, V79, HCT-15, and HCC1937) is inhibited by YCH1899 (3.5 h), with IC50s ranging from 1.19 to 44.24 nM[1]. Capan-1, Capan-1/OP, and Capan-1/TP cells are exposed to 1 μM of YCH1899 for 24 hours, which causes DNA damage and significantly increases the amount of γH2AX [1]. When administered at a concentration of 1 μM for 48 hours, YCH1899 significantly lowers the repair activity of homologous recombination (HR) in U2OS-DR-GFP cells [1].
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ln Vivo |
In rats, YCH1899 (5 mg/kg, intravenously) exhibits a moderate capacity for scavenging [1]. In a tumor model derived from xenograft mice, YCH1899 in MDA-MB-436/OP (6.25, 12.5, and 25 mg/kg, given orally once daily for 27 days) and Capan-1/R (12.5 and 25 mg/kg, given orally once daily, lasting 21 days) overcome Talazoparib resistance and markedly decreased tumor volume [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HCC1937, HCT-15, MDA-MB-436, UWB1.289, UWB1.289+BRCA1, V–C8, V79 cells Tested Concentrations: 0-1 μM approximately Incubation Duration: 24 h Experimental Results: 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 Types: Capan-1, Capan-1/OP cells, Capan-1/TP cells Tested Concentrations: 0.01, 0.1, 1 μM Incubation Duration: 24 h Experimental Results: Increased γH2AX level in a dose-dependent manner. Western Blot Analysis[1] Cell Types: Capan-1 and Capan-1/ OP cells Tested Concentrations: 1, 10, 100 nM Incubation Duration: 4 h Experimental Results: 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 . |
Animal Protocol |
Animal/Disease Models: MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice[1]
Doses: 12.5 and 25 mg/kg Route of Administration: Oral administration Experimental Results: 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/Disease Models: rats[1 ] Doses: 5 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h). |
References |
[1]. Sun Y, et al. YCH1899, a Highly Effective Phthalazin-1(2H)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors. J Med Chem. 2023 Aug 21.
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Molecular Formula |
C25H18BRFN6O3
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Molecular Weight |
549.35
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 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 | |
10 mM | 0.1820 mL | 0.9102 mL | 1.8203 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.