Ilorasertib hydrochloride ABT-348 hydrochloride|cas:1847485-91-9|西域试剂

Ilorasertib hydrochloride ABT-348 hydrochloride,99.67%

产品编号：Bellancom-16018A| CAS NO：1847485-91-9| 分子式：C₂₅H₂₂ClFN₆O₂S| 分子量：525.00

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16018A	￥800.00	杭州北京（现货）
Bellancom-16018A	￥1600.00	杭州北京（现货）
Bellancom-16018A	￥2600.00	杭州北京（现货）
Bellancom-16018A	￥9500.00	杭州北京（现货）
Bellancom-16018A	￥16000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Ilorasertib hydrochloride ABT-348 hydrochloride

产品介绍

Ilorasertib (ABT-348) hydrochloride 是一种有效的，具有口服活性和 ATP 竞争性的 aurora 抑制剂，对 aurora A, aurora B, aurora C 的 IC₅₀ 值分别为 116, 5, 1 nM。Ilorasertib hydrochloride 也是一种有效的 VEGF 和 PDGF 抑制剂。Ilorasertib hydrochloride 具有用于急性髓系白血病 (AML) 和骨髓增生异常综合征 (MDS) 的研究潜力。

生物活性

Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC₅₀s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

体外研究

Ilorasertib hydrochloride (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells.
Ilorasertib hydrochloride (1-1000 nM) shows antiproliferative activity.

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

Cell Viability Assay

Cell Line:	H1299, H460 cells
Concentration:	0, 3, 10, 30 nM
Incubation Time:	24 h
Result:	Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC₅₀S of 5, 10 nM for H1299, H460 cells, respectively.

Cell Proliferation Assay

Cell Line:	MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells
Concentration:	1-1000 nM
Incubation Time:
Result:	Showed antiproliferative activity with IC₅₀s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively.

体内研究
(In Vivo)

Ilorasertib hydrochloride (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in MV-4-11 tumor-bearing SCID mice with TGI of 80%, 86%, 94% at 6.25, 12.5, 25 mg/kg, respectively.
Ilorasertib hydrochloride (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively.
Ilorasertib hydrochloride (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells.
Ilorasertib hydrochloride (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse.
Ilorasertib hydrochloride (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse.

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

Animal Model:	Female SCID/beige mice
Dosage:	25 mg/kg
Administration:	Subcutaneous minipump; 24 h
Result:	Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.

Animal Model:	22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))
Dosage:	20 mg/kg
Administration:	P.o.; once weekly for 3 weeks
Result:	Inhibited the tumor growth in mouse.

体内研究

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

Animal Model:	Female SCID/beige mice
Dosage:	25 mg/kg
Administration:	Subcutaneous minipump; 24 h
Result:	Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.

Animal Model:	22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))
Dosage:	20 mg/kg
Administration:	P.o.; once weekly for 3 weeks
Result:	Inhibited the tumor growth in mouse.

体内研究

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

Animal Model:	Female SCID/beige mice
Dosage:	25 mg/kg
Administration:	Subcutaneous minipump; 24 h
Result:	Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.

Animal Model:	22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))
Dosage:	20 mg/kg
Administration:	P.o.; once weekly for 3 weeks
Result:	Inhibited the tumor growth in mouse.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (79.37 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9048 mL	9.5238 mL	19.0476 mL
5 mM	0.3810 mL	1.9048 mL	3.8095 mL
10 mM	0.1905 mL	0.9524 mL	1.9048 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (3.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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