Exatecan mesylate

한글명:Exatecan mesylate

카스 번호169869-90-3

상품명:Exatecan mesylate

CBNumberCB62526191

분자식C25H26FN3O7S

포뮬러 무게531.56

MOL 파일169869-90-3.mol

화학적 성질

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
색상	Light yellow to green yellow
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\|

그림문자(GHS)

그림문자(GHS)
신호 어

Danger
유해·위험 문구

H301：삼키면 유독함

H315：피부에 자극을 일으킴

H319：눈에 심한 자극을 일으킴

H335：호흡 자극성을 일으킬 수 있음
예방조치문구

P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

P264：취급 후에는 손을 철저히 씻으시오.

P264：취급 후에는 손을 철저히 씻으시오.

P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

P301+P310：삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

P302+P352：피부에 묻으면 다량의 물로 씻으시오.

P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

P321：(…) 처치를 하시오.

P330：입을 씻어내시오.

P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

P337+P313：눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.

P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

P405：밀봉하여 저장하시오.

P501：...에 내용물 / 용기를 폐기 하시오.

Exatecan mesylate 화학적 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 공급 업체

Send Inquriy