human multiple myeloma tumor

GSK467 是一种有效的、选择性的 KDM5 (JARID1) 抑制剂，Ki 值为10 nM。

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Tumour-associated MUC1 epitope是一种具有标志性的生物活性肽。作为高度糖基化的I型跨膜糖蛋白MUC1的一部分，该肽通过特定的胞外结构域展现，该结构域包含20个氨基酸组成的可变数量串联重复序列(VNTR)。在多种人类腺癌及血液恶性肿瘤（如多发性骨髓瘤和B细胞淋巴瘤）中细胞表面表达过量，因此，MUC1是许多免疫治疗策略的关键靶点。