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Exatecan Mesylate Has Antitumor Activity

Exatecan Mesylate Has Antitumor Activity

English name：Exatecan mesylate
CAS number：169869-90-3
Another name:
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
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Products Description

 

English name：Exatecan mesylate

CAS number：169869-90-3

Molecular formula: C25H26FN3O7S

Molecular weight: 531.56

EINECS not have

Related categories:

ADC toxin drug; cytotoxin; chemical reagent; other

 

Structural formula:

1 -

 

Ictecan mesylate

Storage conditions: 4 C, protectfromlight, storedundernitrogen

Solubility: DMSO: 7.41 (maximum concentration mg / ChemicalbookmL); 13.94 (maximum concentration mM) Water: 0.0 (maximum concentration mg/mL); 0.19 (maximum concentration mM)

Form: solid

Color: Light yellow to yellow-green

Stability: Hygroscopicity

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|

 

Icitecan mesylate, use and synthesis method

 

Use

Icetecan mesylate is a DNA topoisomerase I (topoisomerase I) inhibitor with a IC50 of 2.2 μ M (0.975 μg/mL) and can be used in cancer studies.

 

Bioactivity

Exatecan mesylate (DX8951f) is a DNA topoisomerase I (topoisomerase I) inhibitor with a IC50 value of 2.2 μ M (0.975 μ g / mL) and can be used in cancer research.

 

Target spot

Topoisomerase I 0.975 μ g/mL (IC 50)

 

In vitro study

Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC 50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC 50 s of 1.43 nM-4.07 nM, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC 50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC 50 , >10,000 ng/mL).

 

In vivo research

Exatecan mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.

 

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