SEL24-B489|cas:1616359-00-2|西域试剂

SEL24-B489,98.58%

产品编号：Bellancom-120758| CAS NO：1616359-00-2| 分子式：C₁₅H₁₈Br₂N₄O₂| 分子量：446.14

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-120758		￥5000.00	杭州北京（现货）
Bellancom-120758		￥8500.00	杭州北京（现货）

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SEL24-B489

产品介绍

SEL24-B489 是有效的、I 型的、口服有效的、PIM 和 FLT3-ITD 的双抑制剂，其对PIM1、PIM2 和 PIM3 的 K_d 值分别为 2 nM、2 nM、和 3 nM。

生物活性

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.

体外研究

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 (Ser⁷²⁶) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage.

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

Cell Viability Assay

Cell Line:	AZD1208, AC220 and AraC in AML cell lines.
Concentration:	0-10 μM.
Incubation Time:	72 h.
Result:	Decreased viability.

体内研究
(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.

西域 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).

体内研究

西域 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).

体内研究

西域 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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (56.04 mM; ultrasonic and adjust pH to 2 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2414 mL	11.2072 mL	22.4145 mL
5 mM	0.4483 mL	2.2414 mL	4.4829 mL
10 mM	0.2241 mL	1.1207 mL	2.2414 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。-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 (5.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.60 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