货号	规格	价格	上海	北京	珠海	重庆	武汉
S89394-5mg买3赠1	98.90%	￥370.00 S89394-5mg ￥370.00 现货（买3赠1）	5 5	-	-	-	-
S89394-10mg买3赠1	98.90%	￥600.00 S89394-10mg ￥600.00 现货（买3赠1）	4 4	-	-	-	-
S89394-25mg促销	98.90%	￥1200.00 ￥960.00 S89394-25mg ￥960.00 现货	5 5	-	-	-	-
S89394-100mg促销	98.90%	￥3070.00 ￥2450.00 S89394-100mg ￥2450.00 现货	2 2	-	-	-	-

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产品描述：

Farudodstat(LAS 186323,ASLAN003) 是一种有效的 DHODH (Dihydroorotate dehydrogenase) 的口服抑制剂，对人DHODH酶的IC50值为35 nM。ASLAN003 可通过激活 AP-1 转录因子来破坏急性髓性白血病(AML)细胞中的蛋白质合成并诱导其分化和凋亡转录程序

靶点：

AP-1; human DHODH(Cell-free assay):35 nM;Apoptosis; Dehydrogenase; DNA/RNASynthesis

体外研究：

ASLAN003 is a highly potent dihydroorotate dehydrogenase inhibitor that induces differentiation, as well as reducing cell proliferation and viability, of AML cell lines and primary AML blasts including chemoresistant cells. Apoptotic pathways are triggered by ASLAN003, and this drug also significantly inhibits protein synthesis and activates AP-1 transcription, contributing to its capacity to promote differentiation

体内研究：

ASLAN003 substantially reduces leukemic burden and prolongs survival in AML xenograft mice and AML patient-derived xenograft models. ASLAN003 has no evident effect on normal hematopoietic cells and exhibits excellent safety profiles in mice, even after a prolonged period of administration

细胞实验：

Cell lines: MOLM-14 cells, KG-1 cells Concentrations: 1 μM, 2 μM Incubation Time: 1 h Method: Click-iT assays are performed using an O-propargylpuromycin (OPP) Alexa Fluor® 488 Protein Synthesis Assay Kit according to the manufacturer’s recommendation. MOLM-14 and KG-1 cells are exposed to ASLAN003 1 μM or 2 μM for 1 h before OPP 20 mM was added for 1 h. DMSO is used as a control. Cells are washed in ice-cold phosphate-buffered saline and then fixed and permeabilized prior to FACS analysis using a LSRII flow cytometer.

动物实验：

Animal Models: 4-6 week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ, NGS mice Dosages: 50 mg/kg Administration: Oral gavage

参考文献：

1. Jianbiao Zhou, et al. ASLAN003, a potent dihydroorotate dehydrogenase inhibitor for differentiation of acute myeloid leukemia. Haematologica. 2019 Nov7;haematol.2019.230482.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.806 ml	14.032 ml	28.064 ml
5 mM	0.561 ml	2.806 ml	5.613 ml
10 mM	0.281 ml	1.403 ml	2.806 ml
50 mM	0.056 ml	0.281 ml	0.561 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

ASLAN003

2-((3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)amino)nicotinic acid

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)