TNIK-IN-3
Based on 1 Customer Validation
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.79%
- CAS 番号: 2754265-25-1
- 分子式: C23H18FN3O2
- 分子量:387.41
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
IC50: 0.026 μM (TNIK)[1], 0.030 μM (Flt4)[1], 0.191 μM (Flt1)[1], 0.411 μM (DRAK1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
8 μM
Compound: 21k
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Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
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[PMID: 34985886] |
| HCT-116 | IC50 |
4.26 μM
Compound: 21k
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
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[PMID: 34985886] |
TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively[1].
TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively[1].
TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells[1].
TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells[1].
TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells[1].
TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and DLD-1 cells
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Concentration:0.1-100 μM
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Incubation Time:3 days
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Result:Inhibited cell viability in a dose-dependent manner.
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Cell Line:HCT116 cells
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Concentration:5, 10, 20, 40 μM
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Incubation Time:48 hours
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Result:Inhibited the expression of Wnt target genes AXIN2 and c-Myc, LRP5 and LRP6 proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old female NOD-SCID mice were injected with HCT116 cells[1]
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Dosage:100, 150 mg/kg
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Administration:P.o. twice daily for 18 days
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Result:Significantly inhibited tumor growth at a dose of 150 mg/kg.
No obvious weight loss and no other side effects were observed.
化学情報
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CAS 番号 2754265-25-1
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性状 Solid
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分子量 387.41
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分子式 C23H18FN3O2
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Color Off-white to light yellow
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SMILES
O=C1C2=CC=C(C=C2OCCN1CC3=CC=C(C=C3)F)C4=CC5=C(NC=C5)N=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 83.33 mg/mL (215.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 2.5812 mL | 12.9062 mL | 25.8124 mL | 64.5311 mL |
| 5 mM | 0.5162 mL | 2.5812 mL | 5.1625 mL | 12.9062 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5812 mL | 6.4531 mL | |
| 15 mM | 0.1721 mL | 0.8604 mL | 1.7208 mL | 4.3021 mL | |
| 20 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2266 mL | |
| 25 mM | 0.1032 mL | 0.5162 mL | 1.0325 mL | 2.5812 mL | |
| 30 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1510 mL | |
| 40 mM | 0.0645 mL | 0.3227 mL | 0.6453 mL | 1.6133 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2906 mL | |
| 60 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3227 mL | 0.8066 mL | |
| 100 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6453 mL |