Farudodstat ASLAN003|cas:1035688-66-4|西域试剂

Farudodstat ASLAN003,99.70%

产品编号：Bellancom-129239| CAS NO：1035688-66-4| 分子式：C₁₉H₁₄F₂N₂O₃| 分子量：356.32

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-129239	￥550.00	杭州北京（现货）
Bellancom-129239	￥900.00	杭州北京（现货）
Bellancom-129239	￥1900.00	杭州北京（现货）
Bellancom-129239	￥3100.00	杭州北京（现货）
Bellancom-129239	￥5000.00	杭州北京（现货）

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Farudodstat ASLAN003

产品介绍

Farudodstat (ASLAN003) 是一种具有口服活性，有效的二氢乳清酸脱氢酶 (DHODH) 抑制剂，对人 DHODH 酶的 IC₅₀ 为 35 nM。Farudodstat 通过激活 AP-1 转录因子来抑制蛋白质合成。Farudodstat 可以诱导凋亡 (apoptosis)，并在急性髓样白血病 (AML) 异种移植小鼠中大大延长其生存期。

生物活性

Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC₅₀ of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

体外研究

Farudodstat (0.01-100 μM; for 48 hours) inhibits leukemic cell proliferation. The cell viability is maintained at ~50% at Farudodstat 1 μM and higher.
Farudodstat (0.5, 1 μM; for 48 hours) significantly increases cleaved caspase 8.
Farudodstat (2, 4 μM; for 96 hours) decreases viability and induces differentiation in primary acute myeloid leukemia blasts and myelodysplastic syndrome samples.
Farudodstat (1, 2 μM; pretreatment 1 h before OPP for 1 h) inhibits protein synthesis, as demonstrated by the reduced incorporation of O-propargyl-puromycin (OPP) at protein translation sites in both MOLM-14 and KG-1 cells. Farudodstat causes the downregulation of EIF4B, and RPL6 proteins.

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

Cell Proliferation Assay

Cell Line:	THP-1, MOLM-14 and KG-1 cells
Concentration:	0.01, 0.1, 1, 10, 100 μM
Incubation Time:	For 48 hours
Result:	Inhibited leukemic cell proliferation of THP-1, MOLM-14 and KG-1 with IC₅₀ values of 152 nM, 582 nM, and 382 nM, respectively.

Western Blot Analysis

Cell Line:	KG-1 and MOLM-14 cells
Concentration:	0.5, 1 μM
Incubation Time:	For 48 hours
Result:	Significantly increased cleaved caspase 8, increased leakage of cytochrome c from mitochondria into the cytosol and induced cleaved caspase-3 and -7.

体内研究
(In Vivo)

Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival.

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

Animal Model:	Female NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells
Dosage:	50 mg/kg
Administration:	Oral gavage; once daily; from the day 3 to 30
Result:	Substantially reduced the number of disseminated tumors and the size of these tumors. Survival was significantly prolonged.

体内研究

Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival.

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

Animal Model:	Female NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells
Dosage:	50 mg/kg
Administration:	Oral gavage; once daily; from the day 3 to 30
Result:	Substantially reduced the number of disseminated tumors and the size of these tumors. Survival was significantly prolonged.

体内研究

Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival.

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

Animal Model:	Female NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ, NGS mice (4-6 weeks old) with MOLM-14 cells
Dosage:	50 mg/kg
Administration:	Oral gavage; once daily; from the day 3 to 30
Result:	Substantially reduced the number of disseminated tumors and the size of these tumors. Survival was significantly prolonged.

性状

Solid

溶解性数据

In Vitro:

DMSO : 130 mg/mL (364.84 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8065 mL	14.0323 mL	28.0647 mL
5 mM	0.5613 mL	2.8065 mL	5.6129 mL
10 mM	0.2806 mL	1.4032 mL	2.8065 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: ≥ 2.17 mg/mL (6.09 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (6.09 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 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% corn oil
Solubility: ≥ 2.17 mg/mL (6.09 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (6.09 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 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。