UM-164
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- CAS號:
- 903564-48-7
- 英文名:
- 903564-48-7
- 英文別名:
- UM-164;CS-2793;DAS-DFGO-II;UM164;UM-164;UM 164;UM-164 (DAS-DFGO-II);UM-164 trifluoroacetate salt;p38 MAPK,Autophagy,UM-164,Src,UM 164,inhibit,Inhibitor;2-((6-(4-(2-Hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)thiazole-5-carboxamide;2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide;5-Thiazolecarboxamide, 2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-
- 中文名:
- UM-164
- 中文別名:
- 化合物UM-164;化學(xué)試劑/UM-164;2-((6-(4-(2-羥乙基)哌嗪-1-基)-2-甲基嘧啶-4-基)氨基)-N-(2-甲基-5-(3-(三氟甲基)苯甲酰氨基)苯基)噻唑-5-甲酰胺;2-[[6-[4-(2-羥基乙基)-1-哌嗪基]-2-甲基-4-嘧啶基]氨基]-N-[2-甲基-5-[[3-(三氟甲基)苯甲?；鵠氨基]苯基]-5-噻唑甲酰胺
- CBNumber:
- CB54033656
- 分子式:
- C30H31F3N8O3S
- 分子量:
- 640.68
- MOL File:
- 903564-48-7.mol
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UM-164化學(xué)性質(zhì)
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密度:
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1.433±0.06 g/cm3(Predicted)
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儲存條件:
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Store at -20°C
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溶解度:
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DMSO: 5 mg/ml
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形態(tài):
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A crystalline solid
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酸度系數(shù)(pKa):
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11.40±0.70(Predicted)
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顏色:
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White to off-white
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水溶解性:
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H2O: 10mg/mL, clear
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UM-164性質(zhì)、用途與生產(chǎn)工藝
UM-164 (DAS-DFGO-II) 是一種高效的 c-Src 抑制劑，Kd 為 2.7 nM。UM-164 還高效抑制 p38α 和 p38β 活性。
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p38α
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p38β
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c-Src
2.7 nM (Kd)
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In biochemical assays, UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 K
d
=2.7 nM, Dasatinib K
d
=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 G
0
-G
1
cells by 25% and 28%, respectively, and concurrently decreased the fraction of S cells by 16% and 19%, respectively.
A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 and SUM 149 cell lines. Once the tumors become palpable, the mice are randomized into control and treatment groups. Mice are injected intraperitoneally with either drug (10 and 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164, there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg and 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 and P<0.004, respectively).
用途
一種有效的C-SRC/p38激酶抑制劑。UM-164 is a potent dual c-Src/p38 kinase inhibitor that exhibits potent anti-TNBC activity in xenograft models. UM-164 inhibits p38 kinase and binds to an inactive c-Src conformation. UM-164 has a high therapeutic index in vivo.
UM-164
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價(jià)格 |
|---|
| 2025/05/22 | HY-112182 | UM-164 | 903564-48-7 | 1 mg | 323元 |
| 2025/05/22 | HY-112182 | UM-164
UM-164 | 903564-48-7 | 5mg | 850元 |
903564-48-7, UM-164 相關(guān)搜索:
- 抑制劑
- 藥靶配體
- 標(biāo)準(zhǔn)品
- C30H31F3N8O3S
- 化學(xué)試劑/UM-164
- 2-((6-(4-(2-羥乙基)哌嗪-1-基)-2-甲基嘧啶-4-基)氨基)-N-(2-甲基-5-(3-(三氟甲基)苯甲酰氨基)苯基)噻唑-5-甲酰胺
- 化合物UM-164
- 2-[[6-[4-(2-羥基乙基)-1-哌嗪基]-2-甲基-4-嘧啶基]氨基]-N-[2-甲基-5-[[3-(三氟甲基)苯甲酰基]氨基]苯基]-5-噻唑甲酰胺
- 903564-48-7
- 2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide
- UM-164 trifluoroacetate salt
- 2-((6-(4-(2-Hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)thiazole-5-carboxamide
- p38 MAPK,Autophagy,UM-164,Src,UM 164,inhibit,Inhibitor
- 5-Thiazolecarboxamide, 2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-
- UM-164 (DAS-DFGO-II)
- UM164;UM-164;UM 164
- CS-2793
- DAS-DFGO-II
- UM-164