BVB-808 is a selective Jak2 type 1 inhibitor. Janus kinases are critical components of signaling pathways that regulate hematopoiesis. Mutations of the non-receptor tyrosine kinase JAK2 are found in many BCR-ABL-negative myeloproliferative neoplasms. Preclinical results support that JAK2 inhibitors could show efficacy in treating chronic myeloproliferative neoplasms. JAK2 has also been postulated to play a role in BCR-ABL signal transduction. Therefore, inhibitors of JAK2 kinases are turning into therapeutic strategies for treatment of chronic myelogenous leukemia (CML).
Interleukin-6 fragment (human) 是一种多效性细胞因子,由淋巴细胞及非淋巴细胞产生。该分子的编码基因位于人类第7号染色体,长度大约为5 kb。Interleukin-6 fragment (human) 在免疫响应、急性相应、炎症过程、癌症治疗及血液造血方面均有重要的潜在应用。
Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).
Trimethoprim sulfate is a pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. The interference with folic acid metabolism may cause a depression of hematopoiesis. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM-SULFAMETHOXAZOLE COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.