Exatecan mesylate
|
|
Exatecan mesylate 속성
- 저장 조건
- 4°C, protect from light, stored under nitrogen
- 용해도
- DMSO:7.41(Max Conc. mg/mL);13.94(Max Conc. mM)
Water:0.0(Max Conc. mg/mL);0.19(Max Conc. mM)
- 물리적 상태
- 고체
- 안정성
- 흡습성
- InChIKey
- BICYDYDJHSBMFS-OVCYJQQENA-N
- SMILES
- S(O)(=O)(=O)C.N[C@H]1CCC2C(C)=C(F)C=C3N=C4C5=CC6[C@@](C(=O)OCC=6C(=O)N5CC4=C1C3=2)(O)CC |&1:6,21,r|
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
Exatecan mesylate C화학적 특성, 용도, 생산
개요
Exatecan mesylate is a semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting the religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogs.용도
Exatecan Mesylate (DX8951f) is a topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) for cancer research.Synthesis
The synthesis of Exatecan mesilate is as follows:500mL reaction flask,To a suspension of compound II (15 g, 1.0 eq) in ethylene glycol monomethyl ether (150 mL),After adding methanesulfonic acid (75 mL) and water (75 mL) under cooling,The solution was heated under reflux for 24 hours,The reaction was complete as detected by LCMS and cooled to 25°C.Remove the solvent under reduced pressure, add 2L methanol, stir for 2 hours and filter,The filter cake was washed with 200 mL methanol,Dry to obtain 9g of yellow ixitecan mesylate crude product,Yield 53.9%, HPLC purity: 96%.
Clinical claims and research
Exatecan mesylate is a synthetic camptothecin analog that is a more potent inhibitor of topoisomerase I than camptothecin, topotecan, and the active metabolite of irinotecan (CPT-11), SN-38. In preclinical studies, exatecan mesylate demonstrated broad antitumor activity compared with available camptothecin analogs. Furthermore, the antitumor activity observed in Phase I trials made exatecan mesylate an attractive compound for clinical development. A Phase II trial was designed to further evaluate the activity and pharmacokinetic (PK) profile of exatecan mesylate and determine its toxicity and tolerability in patients with metastatic breast carcinoma treated previously with anthracyclines and taxanes[1-2].Exatecan mesylate 준비 용품 및 원자재
원자재
준비 용품
Exatecan mesylate 공급 업체
글로벌( 161)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| ChemExpress | +86-021-58950125 |
info@chemexpress.com | China | 557 | 58 |
| Shanghai Minbiotech Co., Ltd. | +8617315815539 |
sales@minbiotech.com | CHINA | 129 | 58 |
| Fuxin Pharmaceutical | +86-021-021-50872116 +8613122107989 |
contact@fuxinpharm.com | China | 10297 | 58 |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9348 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32480 | 60 |
| Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 |
figo.gao@foxmail.com | China | 6992 | 58 |
| Shochem(Shanghai) Co.,Ltd | 86-21-50800795 |
info@shochem.com | CHINA | 288 | 58 |
| BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
| ENBRIDGE PHARMTECH CO., LTD. | +8613812269233 |
tinayang@enbridgepharm.com | China | 303 | 58 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 |
contact@trustwe.com | China | 5738 | 58 |