SEL24-B489

CAS: 1616359-00-2 货号: S656385 分子式: C15H18Br2N4O2 分子量: 446.14 EC号: 879-181-0 PubChem CID: 76286825
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
S656385-1ml
期货 Stock Image
¥5,500.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with K d values of 2 nM for PIM1 , 2 nM for PIM2 and 3 nM for PIM3 , respectively

In Vitro

In MOLM-13 and to a lesser extent in MV4-11 cells, a dose-dependent disruption of cell cycle with especially pronounced depletion of the S phase after treatment with SEL24-B489, accompanied by PARP cleavage and apoptosis was observed. SEL24-B489 causes a profound inhibition of S6 (S 235/236 ), but has little effect on PI3K/mTOR signaling. SEL24-B489 inhibits STAT5 (Ser 726 ) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AZD1208, AC220 and AraC in AML cell lines. Concentration: 0-10 μM. Incubation Time: 72 h. Result: Decreased viability.

In Vivo

SEL24-B489 (25-100 mg/kg, orally) exhibited activity in AML in vivo models . SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID/beige mice bearing MV-4-11 tumors (FLT3-ITD+) . Dosage: 50, 75 and 100 mg/kg. Administration: Orally, twice daily. Result: Marked dose – dependent tumor reduction (67%, 74% and 82% tumor growth inhibition (TGI) for 50, 75 and 100 mg/kg daily doses, respectively).

IC50& Target:PIM1 2 nM (Kd) PIM2 2 nM (Kd) PIM3 3 nM (Kd) FLT3-ITD

规格

规格或纯度
10mM in DMSO
英文名称
SEL24-B489
生化机理
SEL24-B489 是一种强效的 I 型口服活性 PIM 和 FLT3-ITD 双抑制剂,对 PIM1 的 K d 值为 2 nM,对 PIM2 的 K d 值为 2 nM,对 PIM3 的 K d 值为 3 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
879-181-0
分子类型
小分子
Isomeric SMILES
CC(C)N1C2=CC(=C(C(=C2N=C1C3CCNCC3)[N+](=O)[O-])Br)Br
关联CAS
PubChem CID
分子量
446.14

技术文档

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高级数据

安全和危险性(GHS)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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