anti-myeloma

DCZ0415 在体外、体内和耐药性骨髓瘤患者的原代细胞中诱导抗骨髓瘤活性。它是一种 TRIP13 抑制剂，可损害非同源末端连接的修复并抑制 NF-κB 活性。

PTC-209 是特定的BMI-1抑制剂，不可逆转地损害结直肠癌起始细胞，在 HEK293T 细胞系中的IC50为 0.5 μM。它有抗骨髓瘤活性并损害肿瘤微环境。

SC99 是一种口服有效选择性STAT3抑制剂，靶向 JAK2-STAT3 途径，抑制血小板活化和聚集，有抗骨髓瘤和抗血栓活性。它结合在 JAK2 的 ATP 结合袋中，抑制 JAK2 和 STAT3 的磷酸化。

Mezigdomide (CC-92480) 是一种有效的、新型的 、具有选择性的和具有活性的cereblon E3 泛素连接酶调节剂(CELMoD)，常以分子胶的方式发挥作用。Mezigdomide 具有抗骨髓瘤活性。[1]

Magrolimab (Hu5F9-G4) 是一种人源化抗 CD47 IgG4 单克隆抗体，通过阻断CD47来展现其抗肿瘤活性，主要与CD47的 N 末端焦谷氨酸结合，可用于和其他化合物联合治疗复发性骨髓瘤。

(S)-Thalidomide ((S)-(-)-Thalidomide) 是 Thalidomide 的 S 型异构体，具有免疫调节，抗炎，抗癌，抗血管生成活性和促凋亡活性，可用于研究麻风结节性红斑和骨髓瘤。

Icaritin (Anhydroicaritin) 是Epimedium Genusis 的异戊二烯类黄酮衍生物，有效抑制 K562 细胞和原代 CML 细胞的增殖。它可以调节MAPK ERK JNK 和JAK2 STAT3 AKT 信号传导，并具有增强成骨的作用。

CCF642 (AC1LYELL) 是蛋白质二硫键异构酶抑制剂(IC50:2.9 μM)。它在多发性骨髓瘤细胞中引起急性内质网应激，并伴随凋亡诱导的钙释放，表现出广泛的抗多发性骨髓瘤作用。

E64FC26 是一种有效的蛋白质二硫键异构酶 (PDI) 家族泛抑制剂，具有抗肿瘤活性，抑制 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6，可用于研究多发性骨髓瘤和胰腺癌。

(R)-BAY1238097是BAY1238097的R-异构体，其活性相对较低。BAY1238097 是一种针对 BET 蛋白与组蛋白结合的高效选择性抑制剂，在各种急性髓性白血病（AML）和多发性骨髓瘤（MM）模型中显示出显著的抗增殖作用。其高活性是通过下调 c-Myc 水平并随后调节其下游转录组实现的。

Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in m

SLM6, an inhibitor of cyclin-dependent kinase-9 (CDK9), exhibits potent anti-multiple myeloma activity.

Elotuzumab(HuLuc 63) (anti-SLAMF7) 是一种靶向 SLAMF7 受体的单克隆抗体。Elotuzumab (anti-SLAMF7) 是一种直接激活NK细胞并诱导抗体依赖性细胞毒性的化合物，可联合来那度胺和地塞米松 （Ld） 用于治疗多发性骨髓瘤。

Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂，具有抗肿瘤活性，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。

LSD1 HDAC6-IN-1 is an orally active compound that functions as a dual inhibitor, targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6). This compound demonstrates promising anti-tumor activity and is particularly valuable for research focused on multiple myeloma (MM) [1].

KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].

Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and the ability to induce cell apoptosis. This compound also exhibits strong inhibition of multiple myeloma, with an IC 50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1]

PTC-209 hydrobromide (PTC-209 HBr) 是一种特定的BMI-1抑制剂，能不可逆转地损害结直肠癌起始细胞，也可损害肿瘤微环境，有抗骨髓瘤活性。它在 HEK293T 细胞系中的IC50为 0.5 μM。

HDAC6-IN-10 is a potent and specific HDAC6 inhibitor, exhibiting an IC50 value of 0.73 nM. It demonstrates remarkable selectivity towards HDAC6, with a selectivity range of 144 to 10,941-fold over other HDAC isoforms. Furthermore, HDAC6-IN-10 exhibits notable anti-proliferative effects on multiple myeloma cells [1].

hGGPPS-IN-1 是 C-2 取代的噻吩并嘧啶基双膦酸盐 (C2-ThP-BPs) 的类似物，对人类香叶基香叶基焦磷酸合成酶 (hGGPPS) 具有有效的抑制作用。hGGPPS-IN-1 可选择性诱导多发性骨髓瘤 (MM) 细胞凋亡 (apoptosis)。hGGPPS-IN-1在体内表现出抗骨髓瘤活性。

TAS-117 hydrochloride 是一种选择性的、有效的、口服具有活力的别构 Akt 抑制剂，作用于 Akt1 (IC50: 4.8 nM) 、Akt2 (IC50: 1.6 nM) 和 Akt3 (IC50: 44 nM)。TAS-117 hydrochloride 能够激发抗骨髓瘤活性，增强蛋白酶体抑制诱导的致命内质网应激，可以诱导细胞凋亡和自噬。

hGGPPS-IN-2 是一种 C-2 取代的噻吩并嘧啶基双膦酸盐 (C2-ThP-BPs) 的类似物，是一种有效的人类香叶基香叶基焦磷酸合成酶 (hGGPPS) 抑制剂。hGGPPS-IN-2 能够靶向作用于多发性骨髓瘤 (MM) 细胞，诱导其选择性凋亡 (apoptosis)，并在体内显示出抗骨髓瘤作用。

Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide......

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226 S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.