171335-80-1 Usage
Description
Exatecan, also known as DX-8951, is a hexacyclic chemical compound that is structurally analogous to camptothecin. It is primarily used as a payload in antibody-drug conjugate (ADC) research due to its potent cytotoxic properties. Exatecan mesylate, a derivative of Exatecan, functions as an inhibitor of DNA topoisomerase I, an enzyme that is crucial for DNA replication, transcription, and recombination.
Uses
Used in Pharmaceutical Industry:
Exatecan is used as a cytotoxic agent for its ability to inhibit DNA topoisomerase I, which is essential for various cellular processes such as DNA replication, transcription, and recombination. This inhibition leads to the prevention of cancer cell proliferation and the induction of cell death, making it a promising candidate for the development of targeted cancer therapies.
Used in Antibody-Drug Conjugate (ADC) Research:
Exatecan is used as a potent payload in the development of antibody-drug conjugates (ADCs). These are a type of targeted cancer therapy that combines the specificity of monoclonal antibodies with the cytotoxic properties of chemotherapy drugs. By attaching Exatecan to an antibody that selectively binds to cancer cells, the conjugate can deliver the toxic payload directly to the tumor, minimizing damage to healthy cells and potentially improving treatment outcomes.
Used in Cancer Treatment:
Exatecan is used as a chemotherapeutic agent for the treatment of various types of cancer. Its mechanism of action involves inhibiting DNA topoisomerase I, which disrupts the cancer cell's ability to replicate and transcribe DNA, ultimately leading to cell death. This targeted approach may offer a more effective and less toxic alternative to traditional chemotherapy for certain cancer types.
Biological Activity
Exatecan (DX-8951) is a DNA topoisomerase I (topoisomerase I) inhibitor with IC50 of 2.2 μM (0.975 μg/mL) for cancer research.
in vitro
Exatecan is a potent topoisomerase I inhibitor, with an IC 50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI 50 s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI 50 s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.
in vivo
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.
Check Digit Verification of cas no
The CAS Registry Mumber 171335-80-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,1,3,3 and 5 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 171335-80:
(8*1)+(7*7)+(6*1)+(5*3)+(4*3)+(3*5)+(2*8)+(1*0)=121
121 % 10 = 1
So 171335-80-1 is a valid CAS Registry Number.
InChI:InChI=1/C24H22FN3O4/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/h6-7,16,31H,3-5,8-9,26H2,1-2H3/t16-,24-/m0/s1
