{{cart_num}}
My CartCAS：1039455-84-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
Qty：
Size：
| CAS | 1039455-84-9 |
| Name | COTI-2 |
| Molecular Formula | C19H22N6S |
| Molecular Weight | 366.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 604-604-1 |
| MDL | MFCD28502211 |
| SMILES | S=C(N1CCN(C2=NC=CC=C2)CC1)N/N=C3CCCC4=C\3N=CC=C4 |
| Target Point | p53 |
| Passage | Apoptosis |
| Background | COTI-2 is a third-generation thiocarbazide, an activator of mutant p53. |
| Biological Activity | COTI-2是一种具有口服活性的第三代胺苯硫脲，是突变型p53的激活剂，具有潜在的抗肿瘤活性。[1] |
| In Vitro | COTI-2可促进突变型p53的重折叠、修复野生型p53的功能。在纳摩尔浓度下，COTI-2对各种人源肿瘤细胞系具有活性作用，通过凋亡诱导细胞死亡[1]。COTI-2对200多种癌症中主要信号通路中的激酶没有显著抑制作用，不抑制Hsp90的ATPase活性[2]。 |
| In Vivo | 对移植有HT-29细胞的人源结直肠异种移植瘤模型进行COTI-2给药，给药浓度为10 mg/kg，可抑制肿瘤生长。浓度低至3 mg/kg的COTI-2还可显著地抑制SHP-77 SCLC异种移植瘤的肿瘤生长。此外，它还可延迟U87-MG，MDA-MB-231和OVCAR-3的移植瘤生长。COTI-2在体内的毒副作较少，安全性较高。COTI-2可选择性地靶向多种人源癌细胞(正如体外实验所证明)，而对正常细胞的毒害作用少[2]。 |
| Cell Experiment | 用不同浓度的COTI-2处理SHP-77细胞48小时。然后用1X预冷PBS洗涤细胞两次，用Annexin V和7AAD对细胞进行染色。即将5 μL Annexin V和7AAD加入到细胞中(1 × 105 cells)，室温黑暗条件下孵育15分钟。然后加入400 μL 1X binding buffer。[2] |
| Animal Experiment | Animal Models: NCr-nu mice; Dosages: 10 mg/kg; Administration: i.p.[2] |
| Data Literature Source | [1] Vladimir J N Bykov，et al. Nature Reviews Cancer. 2017. [2] Kowthar Y Salim，et al. Oncotarget. 2016，7(27): 41363-41379. |
| Unit | Bottle |
| Specification | 5mg 10mg |
COTI-2是第三代胺苯硫脲，是突变型p53的激活剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
