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My CartCAS：2068-78-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 2068-78-2 |
| Name | Vincristine sulfate |
| Molecular Formula | C46H58N4O14S |
| Molecular Weight | 923.04 |
| Solubility | Soluble in Water/DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 218-190-0 |
| MDL | MFCD00084729 |
| SMILES | CC[C@@]1(C=CCN2CC3)[C@@]2([H])[C@@]3(C4=CC([C@](C5=C6C7=CC=CC=C7N5)(C[C@](C[C@](CC)(O)C8)([H])C[N@@]8CC6)C(OC)=O)=C(OC)C=C4N9C=O)[C@]9([H])[C@](C(OC)=O)(O)[C@@H]1OC(C)=O.O=S(O)(O)=O |
| Target Point | Microtubule/Tubulin |
| Passage | Cytoskeleton |
| Background | Vincristine sulfate is an alkaloid that inhibits microtubule formation in the mitotic spindle, resulting in arrest of dividing cells in metaphase. Inhibits microtubule polymerization by binding to tubulin |
| Biological Activity | Vincristine sulfate是一种抗肿瘤长春花生物碱，抑制有丝分裂纺锤体中的 microtubule 形成，导致中期阶段的分裂细胞停滞。 它与 microtubule 结合的 Ki 为85 nM。[1-6] |
| In Vitro | 长春新碱抑制稳态微管组装末端微管蛋白二聚体的净添加，Ki为85 nM [1]。长春新碱稳定心轴装置，导致染色体不能分离，导致中期停滞和低浓度的有丝分裂抑制。在较高浓度下，长春新碱可能会破坏并诱导微管的完全解聚[2]。长春新碱诱导肿瘤细胞凋亡，抑制SH-SY5Y细胞增殖，IC50为0.1μM。长春新碱诱导有丝分裂停滞并促进caspase-3和-9和cyclin B的表达，同时降低cyclin D的表达[3]。长春新碱诱导的神经毒性是由于干扰微管功能引起的，导致轴突运输受阻，从而导致轴突变性[4]。 |
| In Vivo | 长春新碱(3mg / kg，ip)诱导平均生长延迟> 120和> 52天，并且重新填充0.06％和5％的组分，分别在携带双侧皮下异种移植物Rh12或Rh18的小鼠中给药[5]。 |
| Cell Experiment | 将细胞以约5×10 4个细胞/ mL的浓度接种在35mm板中的2mL培养基中，并在37℃，5％CO 2和95％空气的气氛中生长24小时。然后用缺乏或含有4nM药物的新鲜培养基替换培养基，并继续增殖3天。在用胰蛋白酶和EDTA分离细胞后，每天在库尔特计数器中进行细胞计数。 |
| Data Literature Source | [1]. Jordan， M.A.， et al. Comparison of the effects of vinblastine， vincristine， vindesine， and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res， 1985. 45 (6) : p. 2741-7. [2]. Gidding， C.E.， et al， Vincristine revisited. Crit Rev Oncol Hematol， 1999. 29 (3) : p. 267-87. [3]. Donoso， J.A.， et al， Action of the vinca alkaloids vincristine， vinblastine， and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res， 1977. 37 (5) : p. 1401-7. [4]. Horton， J.K.， et al. Relationships between tumor responsiveness， vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. Biochem Pharmacol， 1988. 37 (20) : p. 3995-4000. [5]. Baguley， B.C.， et al， Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer， 1991. 27 (4) : p. 482-7. [6]. Zhang D， et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int J Nanomedicine. 2017 Mar 16; 12:2081-2108. |
| Unit | Bottle |
| Specification | 5mg 10mg 10mM*1mL in DMSO 20mg |
是一种生物碱，抑制有丝分裂纺锤体中的 microtubule 形成，导致中期阶段的分裂细胞停滞。通过与微管蛋白结合而抑制微管聚合
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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