Exatecan mesylate
Exatecan mesylate 物理性質(zhì)
- 貯蔵溫度 :
- 4°C, protect from light, stored under nitrogen
- 溶解性:
- DMSO:7.41(Max Conc. mg/mL);13.94(Max Conc. mM)
Water:0.0(Max Conc. mg/mL);0.19(Max Conc. mM)
- 外見 :
- A solid
- 色:
- Light yellow to green yellow
- 安定性：:
- Hygroscopic
- 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|
安全性情報
- リスクと安全性に関する聲明
- 危険有害性情報のコード(GHS)
| WGK Germany |
WGK 3 |
|
|
| ストレージクラス |
6.1A - Combustible acute toxic Cat. 1 and 2
very toxic hazardous materials |
|
|
| Hazard Classifications |
Acute Tox. 2 Oral
Muta. 1B
Repr. 1B |
|
|
| 絵表示（GHS） |
 
|
| 注意喚起語 |
|
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
區(qū)分 |
注意喚起語 |
シンボル |
P コード |
| H301 |
飲み込むと有毒 |
急性毒性、経口 |
3 |
危険 |
|
P264, P270, P301+P310, P321, P330,P405, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強(qiáng)い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標(biāo)的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
|
|
|
| 注意書き |
| P261 |
粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。 |
| P264 |
取扱い後は皮膚をよく洗うこと。 |
| P264 |
取扱い後は手や顔をよく洗うこと。 |
| P270 |
この製品を使用する時に、飲食または喫煙をしないこ と。 |
| P271 |
屋外または換気の良い場所でのみ使用すること。 |
| P280 |
保護(hù)手袋/保護(hù)衣/保護(hù)眼鏡/保護(hù)面を著用するこ と。 |
| P301+P310 |
飲み込んだ場合：直ちに醫(yī)師に連絡(luò)すること。 |
| P302+P352 |
皮膚に付著した場合：多量の水と石鹸で洗うこと。 |
| P304+P340 |
吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。 |
| P305+P351+P338 |
眼に入った場合：水で數(shù)分間注意深く洗うこと。次にコ ンタクトレンズを著用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
| P312 |
気分が悪い時は醫(yī)師に連絡(luò)すること。 |
| P321 |
特別な処置が必要である（このラベルの．．． を見よ）。 |
| P330 |
口をすすぐこと。 |
|
Exatecan mesylate 価格
| メーカー |
製品番號 |
製品説明 |
CAS番號 |
包裝 |
価格 |
更新時間 |
購入 |
Exatecan mesylate 化學(xué)特性,用途語,生産方法
説明
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.
使用
Exatecan Mesylate (DX8951f) is a topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) for cancer research.
作用機(jī)序
Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting 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 analogues
[3].
合成
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 上流と下流の製品情報
原材料
準(zhǔn)備製品
Exatecan mesylate 生産企業(yè)
Global( 227)Suppliers
169869-90-3()キーワード:
- 169869-90-3
- DX 8951f
- Exatecan Meslate
- 169869-90-3 （free base）
- DX 8951; DX 8951;169869-90-3 (FREE BASE)
- (1S,9S)-1-AMINO-9-ETHYL-5-FLUORO-9-HYDROXY-4-METHYL-2,3,9,10,13,15-HEXAHYDRO-1H,12H-BENZO[DE]PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLINE-10,13-DIONE MESYLATE
- Exatecan (DX-8951) mesylate
- DX8951F;DX 8951F;DX-8951F
- Exatecan?Mesylate top3
- Exatecan Mesylate (DX8951f)
- (1S,9S)-1-amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-2,3,12,15-tetrahydrobenzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13(1H,9H)-dione methanesulfonate
- Exatecan mesylate (DX8951)
- (1S,9S)-1-Amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-2,3,12,15-tetrahydrobenzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13(1H,9H)-dione Mesylate
- Shatikang methanesulfonate
- (1S,9S)-1-amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-1,2,3,9,12,15-hexahydro-10H,13H-benzo[de]pyrano [3',4':6,7]indolizino[1,2-b]quinoline-10,13-dione methanesulfonate
- Exatecan mesylate
- (1S,9S)-1-Amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-2,3,12,15-tetrahydrobenzo[de]pyrano[3’,4’:6,7]indolizino[1,2-b]quinoline-10,13(1H,9H)-dione Mesylate
- Bifendate Impurity 14
- (1s,9s)-1-amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-1,2,3,9,12,15-hexahydro-10h,13h-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13-dione methanesulfonic acid salt
- Exatecan mesilate
- Exatecan,Exatecan Mesylate,Topoisomerase,Inhibitor,inhibit