UM-164
Based on 1 publication(s) in Google Scholar
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
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- 純度 : 98.69%
- CAS 番号: 903564-48-7
- 分子式: C30H31F3N8O3S
- 分子量:640.68
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 UM-164
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生物活性
製品説明
IC50 & Target
[1]|
c-Src 2.7 nM (Kd) |
p38α |
p38β |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1937 | IC50 |
120 nM
Compound: 93; UM-164
|
Anticancer activity against human HCC1937 cells assessed as cell growth inhibition
Anticancer activity against human HCC1937 cells assessed as cell growth inhibition
|
[PMID: 33650861] |
| Hs-578T | IC50 |
9.1 nM
Compound: 93; UM-164
|
Anticancer activity against human Hs-578T cells assessed as cell growth inhibition
Anticancer activity against human Hs-578T cells assessed as cell growth inhibition
|
[PMID: 33650861] |
| MDA-MB-231 | IC50 |
6.1 nM
Compound: 93; UM-164
|
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition
|
[PMID: 33650861] |
| SUM149PT | IC50 |
230 nM
Compound: 93; UM-164
|
Anticancer activity against human SUM149 cells assessed as cell growth inhibition
Anticancer activity against human SUM149 cells assessed as cell growth inhibition
|
[PMID: 33650861] |
体外実験
In biochemical assays, UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 Kd=2.7 nM, Dasatinib Kd=0.7 nM). To confirm that UM-164 is capable of inhibiting the activation of c-Src in vitro, the effect of UM-164 is examined on the c-Src autophosphorylation in two TNBC cell lines (MDA-MB 231 and SUM 149). Inhibition of c-Src autophosphorylation is detected in a concentration- and a time-dependent manner. At 120 minutes, complete abrogation of c-Src autophosphorylation is observed at 50 nM, demonstrating that UM-164 is a potent c-Src inhibitor in vitro. Flow cytometry experiments demonstrate that UM-164 treatment of MDA-MB 231 and SUM 149 increased the proportion of G0-G1 cells by 25% and 28%, respectively, and concurrently decreased the fraction of S cells by 16% and 19%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 903564-48-7
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性状 Solid
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分子量 640.68
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分子式 C30H31F3N8O3S
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Color White to off-white
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SMILES
O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=CC(NC(C5=CC=CC(C(F)(F)F)=C5)=O)=CC=C4C
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別名
DAS-DFGO-II
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
体外:
DMSO : 5 mg/mL (7.80 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)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (7.80 mM); Suspended solution; Need ultrasonic
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)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5608 mL | 7.8042 mL | 15.6084 mL | 39.0210 mL |
| 5 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL | 7.8042 mL |