BAY-2402234-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY-2402234Cat. No.: HY-112645CAS No.: 2225819-06-5分式: CHClFNO分量: 520.84作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (240.00 mM; Need ultrasonic)Mass Solv

2、ent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9200 mL 9.5999 mL 19.1998 mL5 mM 0.3840 mL 1.9200 mL 3.8400 mL10 mM 0.1920 mL 0.9600 mL 1.9200 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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在

3、您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.99 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.99 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.99 mM); Clear solution1/2

4、 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 BAY-2402234个选择性的、氢乳 酸脱氢酶 (DHODH) 的抑制剂，可治疗髓恶性肿瘤 (myeloidmalignancies)。IC50 & Target DHODH 1.体外研究 BAY-2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity. In vitro, it potentlyinhibits proliferation of AM

5、L cell lines in the sub-nanomolar to low-nanomolar range. BAY-2402234 inducesdifferentiation of AML cell lines also in a sub-nanomolar to low-nanomolar range, demonstrating theanticipated mode of action in cellular mechanistic assays 1.体内研究 BAY-2402234 exhibits strong in vivo anti-tumor efficacy in

6、monotherapy in several subcutaneous anddisseminated AML xenografts as well as AML patient-derived xenograft (PDX) models. Target engagementof the novel DHODH inhibitor BAY-2402234 can be observed by increase of tumoral and plasmadihydroorotate levels after treatment with the inhibitor. Consistent wi

7、th the in vitro data BAY-2402234 inducesAML differentiation in vivo as detected by upregulation of differentiation cell surface markers in xenograft andPDX models after treatment with the inhibitor. Furthermore, differentiation-associated transcriptomic changesare evident following a single administ

8、ration of BAY-2402234 in vivo 1.REFERENCES1. Andreas Janzer, et al. Abstract DDT02-04: BAY 2402234: A novel, selective dihydroorotate dehydrogenase (DHODH) inhibitor for thetreatment of myeloid malignancies. AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL.McePdfHeightCaution: Product has not been fully validated for medical applications.F