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
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|
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..…
N-Bromosuccinimide Price
- Product number
- API0010083
- Product name
- EXATECAN MESYLATE
- Purity
- 99.00%
- Packaging
- 5MG
- Price
- $1550
- Updated
- 2021/12/16
- Product number
- CS-2952
- Product name
- Exatecan(mesylate)
- Purity
- 99.91%
- Packaging
- 500mg
- Price
- $2260
- Updated
- 2021/12/16
- Product number
- CS-2952
- Product name
- Exatecan(mesylate)
- Purity
- 99.91%
- Packaging
- 1g
- Price
- $3760
- Updated
- 2021/12/16
- Product number
- CD31003026
- Product name
- ExatecanMesylate
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $1459
- Updated
- 2021/12/16
- Product number
- DC7578
- Product name
- ExatecanMesylate
- Purity
- >99%
- Packaging
- 250mg
- Price
- $2700
- Updated
- 2021/12/16
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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View Lastest Price from Exatecan mesylate manufacturers
- 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