| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
RK-287107 is a potent TNKS/TNKS2 inhibitor (IC50 = 14.4 nM) with >7000-fold selectivity against the PARP1 enzyme, which inhibits WNT-responsive TCF reporter activity and proliferation of human colorectal cancer cell line COLO-320DM. In a mouse xenograft model, RK-287107 also showed dose-dependent inhibition of tumor growth. Tankyrase inhibitors are a new class of anticancer agents, and RK-287107 is a promising lead compound for their development.
| Targets |
Tankyrase-2 ( IC50 = 10.6 nM ); Tankyrase-1 ( IC50 = 14.3 nM )
|
|---|---|
| ln Vitro |
RK-287107 is a novel inhibitor that selectively inhibits tankyrases 1 and 2. In colorectal cancer cells harboring the shortly truncated APC mutations, RK-287107 causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity, and the target gene expression. The growth of APC-mutant (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells is consistently inhibited by RK-287107, but not that of APC-wild (β-catenin-independent) colorectal cancer RKO cells. [1]
|
| ln Vivo |
RK-287107 administered intraperitoneally or orally inhibits the growth of COLO-320DM tumors in NOD-SCID mice. In vivo, RK-287107 inhibits the growth of tumors and the Wnt/β-catenin pathway in xenografted COLO-320DM cells. [1]
|
| Cell Assay |
RK-287107 is applied to cells in triplicate and left on for 120 hours. MTT assays are used to quantify relative cell number. Plotting of the average values occurs after at least two repetitions of the experiment.
|
| Animal Protocol |
6-week-old female NOD.CB17-Prkdcscid/J mice s.c. injected with COLO-320DM cells
100 mg/kg, 150 mg/kg, 300 mg/kg IP, Oral gavage |
| References |
| Molecular Formula |
C22H26F2N4O2
|
|---|---|
| Molecular Weight |
416.4728
|
| Exact Mass |
416.2
|
| Elemental Analysis |
C, 63.45; H, 6.29; F, 9.12; N, 13.45; O, 7.68
|
| CAS # |
2171386-10-8
|
| Related CAS # |
2171386-10-8
|
| Appearance |
Solid powder
|
| SMILES |
C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO
|
| InChi Key |
FZQYCOUBRJEYBC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H26F2N4O2/c23-14-11-16(24)19-18(12-14)28(9-10-29)13-22(19)5-7-27(8-6-22)21-25-17-4-2-1-3-15(17)20(30)26-21/h11-12,29H,1-10,13H2,(H,25,26,30)
|
| Chemical Name |
2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[2H-indole-3,4'-piperidine]-1'-yl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one
|
| Synonyms |
RK 287107; RK-287107; RK287107
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 83~125 mg/mL (199.3~300.2 mM)
Ethanol: ˂1 mg/mL (NaN mM) Water: ˂1 mg/mL (NaN mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4011 mL | 12.0057 mL | 24.0113 mL | |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8023 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4011 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.
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
