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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
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.

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.

Exatecan mesylate Preparation Products And Raw materials

Raw materials

Preparation Products

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Exatecan mesylate Suppliers

Zhejiang Huida Biotech Co., LTD
Tel
0571-89903882 13626641628
Email
jiangnan@huidabiotech.com
Country
China
ProdList
3661
Advantage
58
Anqing Runke Biomedical Technology Co., Ltd.
Tel
0556-5282330 18075373931
Fax
0556-5282330
Email
sales@growingchem.com
Country
China
ProdList
221
Advantage
58
Wuxi enqiao Pharmaceutical Technology Co., Ltd
Tel
0510-83591909 18018392058
Fax
0510-83591909
Email
info@enbridgepharm.com
Country
China
ProdList
180
Advantage
58
Shanghai Minkai Biological Technology Co., Ltd
Tel
021-52919136 17315815539
Email
2804155403@qq.com
Country
China
ProdList
169
Advantage
58
Shanghai Tekanbio Pharm-Tech Co., Ltd.
Tel
021-50896099 18017206244
Fax
QQ:3268640975
Email
sales@tekanbio.com
Country
China
ProdList
99
Advantage
58
Abydos Scientific
Tel
025-84767922 18936879710
Email
sales@abydoscientific.com
Country
China
ProdList
1026
Advantage
58
Shengyang Runze (Beijing) Technology Co.,
Tel
010-010-57302162 17611011830
Email
lyt001@syrz01.com
Country
China
ProdList
167
Advantage
58
Nantong Nuotai Biomedical Technology Co., Ltd.
Tel
0513-+86-0513-82206272 +86-17712268337
Email
479758216@qq.com
Country
China
ProdList
118
Advantage
58
ZHIWE CHEMTECH CO LTD
Tel
021-20221225 13917446399
Fax
QQ:115820162
Email
sales@zhiwe.net
Country
China
ProdList
588
Advantage
61
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
zhangsn@titansci.com
Country
China
ProdList
14113
Advantage
59
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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:


  • 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
  • 169869-90-3
  • C24H22FN3O4CH4O3S