BAY1238097|cas:1564268-08-1|西域试剂

BAY1238097,98.55%

产品编号：Bellancom-112316| CAS NO：1564268-08-1| 分子式：C₂₅H₃₃N₅O₃| 分子量：451.56

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货号	价格	库存与货期
Bellancom-112316	￥1900.00	杭州北京（现货）
Bellancom-112316	￥2900.00	杭州北京（现货）
Bellancom-112316	￥11000.00	杭州北京（现货）
Bellancom-112316	￥19500.00	杭州北京（现货）

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BAY1238097

产品介绍

BAY1238097 是一种有效的、BET 与组蛋白 结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML (急性髓性白血病) 和MM (多发性骨髓瘤) 模型中表现出较强的抗增殖活性 (IC₅₀ 值 <100 nM)。

生物活性

BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC₅₀ <100 nM).

体外研究

BAY 1238097 shows strong inhibitory activity (IC₅₀ < 100 nM) in a TR-FRET assay using BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, the interaction between BRD4 (IC₅₀=63 nM), BRD3 or BRD2 (IC₅₀=609 nM) and H4 (IC₅₀=2430 nM) is inhibited.
BAY 1238097 has in vitro anti-tumour activity in lymphoma models. BAY 1238097 affects the gene expression of GCB DLBCL cells. At the gene level, BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17 are among the top downregulated genes. Beside histone-coding genes, the upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

BAY 1238097 shows strong efficacy in the AML and MM models. BAY 1238097 has in vivo anti-tumour activity in lymphoma models.
BAY 1238097 is well tolerated at 10-15 mg/kg applied daily over 9-14 days in different disease models, with no obvious toxicity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Severe combined immunodeficiency (SCID) female mice (9-12 weeks old) inoculated subcutaneously into the right flank with 5×10⁶ SU-DHL-8 cells/mouse suspended in 0.1 mL of matrigel or with O
Dosage:	15 mg/kg (maximal tolerated dose).
Administration:	Orally daily for 12 days (on day 21 post-tumour inoculation).
Result:	Showed strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. Also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Severe combined immunodeficiency (SCID) female mice (9-12 weeks old) inoculated subcutaneously into the right flank with 5×10⁶ SU-DHL-8 cells/mouse suspended in 0.1 mL of matrigel or with O
Dosage:	15 mg/kg (maximal tolerated dose).
Administration:	Orally daily for 12 days (on day 21 post-tumour inoculation).
Result:	Showed strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. Also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 150 mg/mL (332.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2145 mL	11.0727 mL	22.1455 mL
5 mM	0.4429 mL	2.2145 mL	4.4291 mL
10 mM	0.2215 mL	1.1073 mL	2.2145 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。