アベマシクリブ
アベマシクリブ 物理性質
- 沸点 :
- 689.3±65.0 °C(Predicted)
- 比重(密度) :
- 1.32±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- 4°C, protect from light
- 溶解性:
- insoluble in H2O; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic; ≥6.34 mg/mL in EtOH with gentle warming
- 外見 :
- solid
- 酸解離定数(Pka):
- 7.69±0.10(Predicted)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQJ-0243 |
N-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-1,3-benzodiazol-5-yl)pyrimidin-2-amine |
1231929-97-7 |
250mg |
￥277200 |
2018-12-26 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQJ-0243 |
N-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-1,3-benzodiazol-5-yl)pyrimidin-2-amine |
1231929-97-7 |
1g |
￥698400 |
2018-12-26 |
購入 |
アベマシクリブ 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, サイクリン依存性キナーゼ(CDK)阻害薬
商品名
ベージニオ (日本イーライリリー)
Biochem/physiol Actions
LY2835219 (abemaciclib) was identified via compound and biochemical screening by scientists at Eli Lilly and Company Research Laboratories and selected for its biological activity and highly selective inhibition of the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. The compound was shown to act as a competitive inhibitor of the ATP-binding domain of the CDK4 and CDK6 and to be 14 times more potent against CDK4 than against CDK6. In comparison to palbociclib and ribociclib, abemaciclib shows higher selectivity for the complex CDK4/cyclin D1, with IC50 values five times lower than those of the two other compounds[1].
酵素阻害剤
This oral cell cycle inhibitor (FWfree-base = 506.61 g/mol; FWmesylate-salt =
602.70 g/mol; CAS 1231930-82-7 (mesylate salt) ), also known as
LY2835219 and N-[5-[ (4-ethyl-1-piperazinyl) methyl]-2-pyridinyl]-5-
fluoro-4-[4-fluoro-2-methyl-1- (1-methylethyl) -1H-benzimidazol-6-yl]-2-
pyrimidinamine, targets the cyclin-dependent kinase CDK4, or cyclin D1
(IC50 = 2 nM) and CDK6, or cyclin D3 (IC50 = 6 nM), inhibiting
retinoblastoma (Rb) protein phosphorylation in early G1, thereby arresting
the cell cycle in the G1, suppressing DNA synthesis, and inhibiting cancer
cell growth. LY2835219 inhibits activation of AKT and ERK, but not
mTOR.
アベマシクリブ 上流と下流の製品情報
原材料
EthaniMidaMide, N-(4-broMo-2,6-difluorophenyl)-N'-(1-Methylethyl)-
4-ブロモ-2,6-ジフルオロアニリン
2-ブロモ-5-ピリジンカルボキシアルデヒド 臭化物
1-((6-ブロモピリジン-3-イル)メチル)-4-エチルピペラジン
N-イソプロピルアセトアミド
6-(2-クロロ-5-フルオロピリミジン-4-イル)-4-フルオロ-1-イソプロピル-2-メチル-1H-ベンゾ[D]イミダゾール
1H-ベンズイミダゾール, 4-フルオロ-2-メチル-1-(1-メチルエチル)-6-(4,4,5,5-テトラメチル-1,3,2-ジオキサボロラン-2-イル)-
1-(4-アミノ-3,5-ジフルオロフェニル)エタノン
5-((4-エチルピペラジン-1-イル)メチル)ピリジン-2-アミン
6-ブロモ-4-フルオロ-1-イソプロピル-2-メチル-1H-ベンゾ[D]イミダゾール
1-エチルピペラジン
2,6-ジフルオロアニリン
準備製品
アベマシクリブ 生産企業
Global( 262)Suppliers
1231929-97-7(アベマシクリブ)キーワード:
ラブセルチブ
N-(1-オキソ-2-プロピルペンチル)-2′,2′-ジフルオロ-2′-デオキシシチジン
ゾスキダル三塩酸塩
LY2584702
4-(3-ピリジン-2-イル-1H-ピラゾール-4-イル)キノリン
(2S)-2-[(2S)-2-(3,5-ジフルオロフェニル)-2-ヒドロキシアセトアミド]-N-[(10S)-8-メチル-9-オキソ-8-アザトリシクロ[9.4.0.02,7]ペンタデカ-1(15),2,4,6,11,13-ヘキサエン-10-イル]プロパンアミド
(S)-4-(2,4-ジフルオロ-5-(ピリミジン-5-イル)フェニル)-4-メチル-5,6-ジヒドロ-4H-1,3-チアジン-2-アミン
2-モルホリノ-8-フェニルクロモン
ガルニセルチブ
- 1231929-97-7
- Abemaciclib, >=98%
- Abemaciclib
- abemaciclib(CDK 4/6 inhibitor)
- Bemaciclib(LY2835219, abemaciclib)
- CDK4/6 dual inhibitor
- LY 2835219 (free base)
- LY2835219 (free base)
- LY-2835219 (free base)
- Bemaciclib(LY2835219free base
- N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine
- LY2835219(Abemaciclib)
- 2-Pyrimidinamine,N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-
- ethyl-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-amine
- LY2835219free base,Abemaciclib
- Abemaciclib free base
- ABEMACICLIB BASE
- Abemaciclib Mesylate (Verzenio)
- CS-814
- LY2835219;LY-2835219;LY 2835219;ABEMACICLIB;CDK4/6 DUAL INHIBITOR;LY-2835219 FREE BASE
- N-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-1,3-benzodiazol-5-yl)pyrimidin-2-amine
- Abemaciclib D10
- Abemaciclib D7
- Abemaciclib (LY2835219)
- N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine
- N-(5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine
- inhibit,LY-2835219,LY 2835219,Abemaciclib,Inhibitor,Cyclin dependent kinase,CDK
- 5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3H-benzimidazol-5-yl)pyrimidin-2-yl)amine
- Abemaciclib Powder
- abecilee
- アベマシクリブ
- アベマシクリブ (JAN)
- 6-[2-[[5-(4-エチルピペラジン-1-イルメチル)ピリジン-2-イル]アミノ]-5-フルオロピリミジン-4-イル]-1-イソプロピル-2-メチル-4-フルオロ-1H-ベンゾイミダゾール
- N-[5-[(4-エチル-1-ピペラジニル)メチル]-2-ピリジル]-5-フルオロ-4-(4-フルオロ-1-イソプロピル-2-メチル-1H-ベンゾイミダゾール-6-イル)ピリミジン-2-アミン
- ベージニオ
- N-{5-[(4-エチルピペラジン-1-イル)メチル]ピリジン-2-イル}-5-フルオロ-4-[4-フルオロ-2-メチル-1-(プロパン-2-イル)-1H-1,3-ベンゾジアゾール-6-イル]ピリミジン-2-アミン
- ベージニオ錠