vinblastine

Vinblastine 抑制微管形成并抑制 nAChR 活性，IC50 为 8.9 μM，用于治疗某些类型的癌症。

Vinblastine sulfate (Vincaleukoblastine sulfate salt) 是对各种癌症类型有细胞毒性的生物碱。 它可以抑制微管的形成，也可以抑制 nAChR，IC50值为8.9 μM。

Pristinamycin IA (Mikamycin B) 是 P-糖蛋白的底物，也是一种环肽类大环内酯抗生素。

MC-Val-Cit-PAB-vinblastine is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), featuring vinblastine (a microtubule protein inhibitor) connected through the MC-Val-Cit-PAB ADC linker.

Vindesine sulfate (Desacetyl Vinblastine amide) 是一种长春花生物碱，它是长春碱的合成衍生物，与有丝分裂纺锤体的微管蛋白结合，导致微管结晶和有丝分裂停滞或细胞死亡。

Desacetylvinblastine (4-Desacetylvinblastine) 是长春碱的关键代谢产物和强效细胞毒性剂。虽然 Desacetylvinblastine 自身的抗肿瘤效果不理想，但在与特定共轭物结合时能够展现出显著的抗肿瘤活性。

Deacetylvinblastine hydrazide, a cytotoxic vinca alkaloid often conjugated with folic acid to produce EC145, a novel folate-receptor targeted agent.

3',4'-Anhydrovinblastine (3',4'-Anhydrovinblastine) 是一种提取自Catharanthus roseus 叶片的单萜吲哚生物碱。

Vinorelbine ditartrate (KW-2307) 属于天然生物碱，是一种抗有丝分裂剂。Vinorelbine ditartrate 具有抗肿瘤活性，可以抑制细胞增殖，诱导细胞凋亡。

Cevipabulin (TTI-237) 是一种微管活性的、口服有效的抗肿瘤化合物，可抑制 [3H] 长春碱与微管蛋白的结合，对人癌细胞的 IC50 值为 18-40 nM。

Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

EC0489, Small molecule-drug conjugate (SMDC) ,a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor.

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

BE-10988 是一种抑制 DNAtopoisomerase 的化合物。该化合物通过促进 DNA 拓扑异构复合物的形成，有效阻断了在对 Doxorubicin 和 长春新碱 显示耐药性的 P388 小鼠白血病细胞系中的细胞增殖。

Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range

ALB-109564 dihydrochloride 是长春碱生物碱的半合成衍生物，是一种微管蛋白抑制剂和抗肿瘤药物。它与微管蛋白单体结合并抑制微管的形成，导致有丝分裂纺锤体组装的破坏和肿瘤细胞停滞在细胞周期的G2/M 期。

A 30312 is a fused indole, which overcomes multidrug resistance in P388 Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.

Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50= 29 μM).2It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3

Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 |Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. Chem.Biol. 18 679 PMID:21700202

C2 Adamantanyl globotriaosylceramide (AdaGb3) is a bioactive sphingolipid and water-soluble form of globotriaosylceramide that contains an adamantanyl group in place of the fatty acyl chain. It inhibits Vero toxin binding to globotriaosylceramide in an ELISA assay when used at a concentration of 10 μM. AdaGb3 decreases cell surface expression of P-glycoprotein (P-gp) and reduces efflux of rhodamine 123 in MDCK cells. It also increases apical-to-basal transport of vinblastine in human intestinal C2BBe1 cells.

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......

Odorine has potent anti-carcinogenic effect by inhibiting both the initiation and promotion stages of two-stage skin carcinogenesis. It was found to inhibit the growth of the vinblastine-resistant KB cells by enhancing the anticancer activity of vinblastine.

Torilin 是一种睾酮5α还原酶抑制剂，它（IC50=31.7+ -4.23μM）对5α还原酶的抑制作用强于α-亚麻酸（IC50=160.3+ -24.62μM），但弱于非那雄胺（IC50=0.38+ -0.06μM）。Torilin 具有免疫调节、肝脏保护和抗炎特性，它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症，它可以减轻关节炎的严重程度，改变 dLN 或关节中的白细胞活化，并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成，IC（50）值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性，它可能通过抑制肿瘤侵袭来抑制肿瘤发生，逆转癌细胞的多药耐药性，它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7 ADR 细胞的细胞毒性。

Isotenulin 刺激 P-糖蛋白 ATPase，从而抑制 P-gp 的外排功能，并克服癌细胞的多药耐药性 (MDR)。它在多药耐药癌细胞 KB-vin 和敏感癌细胞 HeLaS3 中展现了细胞毒性。Isotenulin 与 Paclitaxel、Vinblastine 和 Doxorubicin 具有协同作用。