Motixafortide-BKT140-4-fluorobenzoyl-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMotixafortideCat. No.: HY-P0171CAS No.: 664334-36-5Synonyms: BKT140 (4-fluorobenzoyl); BL-8040; TF14016分式: CHFNOS分量: 2159.52Sequence: 4F-Benzoyl-Arg-Arg-2-Naph-Ala-Cys-Tyr-Cit-Lys-Lys-Pro-Tyr-Arg-Cit-Cys-Arg-NH2 (Disulfide bridg

2、e: Cys4-Cys13)Sequence Shortening: 4F-Benzoyl-RR-2-Naph-Ala-CY-Cit-KKPYR-Cit-CR-NH2(Disulfide bridge: Cys4-Cys13)作靶点: CXCR作通路: GPCR/G Protein; Immunology/Inflammation储存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 36 mg/mL (16.67 mM)* means soluble, but satura

3、tion unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.4631 mL 2.3153 mL 4.6307 mL5 mM 0.0926 mL 0.4631 mL 0.9261 mL10 mM 0.0463 mL 0.2315 mL 0.4631 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。BIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Motixafortide (BKT140

4、4-fluorobenzoyl)种新型的CXCR4拮抗剂，IC50约为1 nM。IC50 & Target CXCR4-1 nM (IC50)体外研究 Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide(BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140)specifically tr

5、iggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulatesapoptotic cell death in leukemia and MM cells 2.体内研究 Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, thegrowth of human acute myeloid leukemia and multipl

6、e myeloma xenografts. Tumors from animals treated withMotixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores2.PROTOCOLCell Assay 2 Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) orAMD3100 for 24 ho

7、urs. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH.Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37C for1 hour,

8、and inactivated by heat treatment (65C for 30 minutes). After incubation, cells are stained withpropidium iodide and the percent of viable PI-negative cells in culture is determined 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Severe c

9、ombined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study.Administration 2 NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 mL per mousecontaining 5106 cells). Tumor growth is monitored daily, and mice are randomized to drug-tre

10、ated or controlPBS-treated groups (10 mice per group) when the tumor size (widthlength) reaches 0.04 cm2. BKT140 isadministered subcutaneously at a dose of 200 mg per mouse each day for 5 days 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES

11、1. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patientswith multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79.2. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011Mar;39(3):282-92.McePdfHeightCaution: Product has no