Exatecan mesylate

Product Name: Exatecan mesylate
CAS No.: 169869-90-3
Chemical Name: Exatecan mesylate
Synonyms: DX 8951f;Exatecan Meslate;Exatecan mesilate;Exatecan mesylate;Bifendate Impurity 14;169869-90-3 （free base）;Exatecan?Mesylate top3;DX8951F;DX 8951F;DX-8951F;Exatecan mesylate (DX8951);Shatikang methanesulfonate
CBNumber: CB62526191
Molecular Formula: C25H26FN3O7S
Formula Weight: 531.56
MOL File: 169869-90-3.mol

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Exatecan mesylate Property

storage temp.: 4°C, protect from light, stored under nitrogen
solubility: DMSO:7.41(Max Conc. mg/mL);13.94(Max Conc. mM)
Water:0.0(Max Conc. mg/mL);0.19(Max Conc. mM)
form: A solid
color: Light yellow to green yellow
Stability:: Hygroscopic
InChI: InChI=1/C24H22FN3O4.CH4O3S/c1-3-24(31)14-6-18-21-12(8-28(18)22(29)13(14)9-32-23(24)30)19-16(26)5-4-11-10(2)15(25)7-17(27-21)20(11)19;1-5(2,3)4/h6-7,16,31H,3-5,8-9,26H2,1-2H3;1H3,(H,2,3,4)/t16-,24-;/s3
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|

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

American Custom Chemicals Corporation

Product number: API0010083
Product name: EXATECAN MESYLATE
Purity: 99.00%
Packaging: 5MG
Price: $1550
Updated: 2021/12/16

ChemScene

Product number: CS-2952
Product name: Exatecan(mesylate)
Purity: 99.91%
Packaging: 500mg
Price: $2260
Updated: 2021/12/16

ChemScene

Product number: CS-2952
Product name: Exatecan(mesylate)
Purity: 99.91%
Packaging: 1g
Price: $3760
Updated: 2021/12/16

Crysdot

Product number: CD31003026
Product name: ExatecanMesylate
Purity: 98+%
Packaging: 5mg
Price: $1459
Updated: 2021/12/16

DC Chemicals

Product number: DC7578
Product name: ExatecanMesylate
Purity: >99%
Packaging: 250mg
Price: $2700
Updated: 2021/12/16

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Exatecan mesylate Chemical Properties,Usage,Production

Description

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.

Uses

Exatecan Mesylate (DX8951f) is a topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) for cancer research.

Mechanism of action

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].

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].

References

[1] M.D., Francisco J. Esteva and Ph.D. “A Phase II study of intravenous exatecan mesylate (DX-8951f) administered daily for 5 days every 3 weeks to patients with metastatic breast carcinoma.” Cancer 98 5 (2003): 900–907.
[2] D. Talbot. “Phase II study of Exatecan Mesylate (DX-8951f) in advanced NSCLC.” Lung Cancer 29 1 (2000): 55.
[3] MESYLATE E. Exatecan Mesylate[J]. Definitions, 2020. DOI:10.32388/vdq0ii.

Exatecan mesylate Preparation Products And Raw materials

Raw materials

Preparation Products

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Exatecan mesylate Suppliers

China 171 United States 9 Global 180

WuYan Pharmaceutical Technology (Shanghai) Co., Ltd.

Tel: 021-61001086 13671938079
Fax: 021-61114075
Email: sales@wuyanpharm.com
Country: China
ProdList: 105
Advantage: 55

Zhejiang Huida Biotech Co., LTD

Tel: 0571-89903882 13626641628
Email: jiangnan@huidabiotech.com
Country: China
ProdList: 3656
Advantage: 58

Wuxi enqiao Pharmaceutical Technology Co., Ltd

Tel: 0510-83591909 18018392058
Fax: 0510-83591909
Email: info@enbridgepharm.com
Country: China
ProdList: 237
Advantage: 58

Shanghai Minkai Biological Technology Co., Ltd

Tel: 021-021-52919136 17315815539
Email: 2804155403@qq.com
Country: China
ProdList: 168
Advantage: 58

Shanghai Tekanbio Pharm-Tech Co., Ltd.

Tel: 021-50896099 18017206244
Fax: QQ：3268640975
Email: sales@tekanbio.com
Country: China
ProdList: 108
Advantage: 58

Abydos Scientific

Tel: 025-84767922 18936879710
Email: sales@abydoscientific.com
Country: China
ProdList: 1009
Advantage: 58

Nantong Nuotai Biomedical Technology Co., Ltd.

Tel: 0513-82206272 17706270880
Email: 479758216@qq.com
Country: China
ProdList: 158
Advantage: 58

Shanghai Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: 021-58955996
Email: info@chemexpress.com
Country: China
ProdList: 815
Advantage: 58

SICHUAN XIELI PHARMACEUTICAL CO.,LTD.

Tel: 028-83188610
Email: info@xielipharm.com
Country: China
ProdList: 29
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ZHIWE CHEMTECH CO LTD

Tel: 021-20221225 13917446399
Fax: QQ:115820162
Email: sales@zhiwe.net
Country: China
ProdList: 627
Advantage: 61

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View Lastest Price from Exatecan mesylate manufacturers

Henan Aochuang Chemical Co.,Ltd.

Product: Exatecan mesilate 169869-90-3
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-10-13

169869-90-3, Exatecan mesylateRelated Search:

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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 mesilate

DX 8951f

Exatecan Meslate

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

Exatecan,Exatecan Mesylate,Topoisomerase,Inhibitor,inhibit

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 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 methanesulfonate

(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

169869-90-3

C24H22FN3O4CH4O3S