Exatecan (DX-8951) |
| Catalog No.GC33108 |
Exatecan (DX-8951) is a nonprodrug camptothecin (CPT) derivative, exhibits significant topoisomerase I inhibition.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 171335-80-1
Sample solution is provided at 25 µL, 10mM.
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Exatecan (DX-8951) is a nonprodrug camptothecin (CPT) derivative, exhibits significant topoisomerase I inhibition [1]. Exatecan (DX-8951) inhibited topoisomerase I with IC50 of 2.2 µM (0.975 µg/ml) [2].
Exatecan (DX-8951) and SN-38 inhibited topoisomerase activity with IC50 values of 0.82 and 2.3 µg/mL, respectively, topoisomerase I was obtained from SUIT-2 cells [3]. Exatecan (DX-8951)(20 ng/ml) induced DNA fragmentation. In an extract from treated SUIT-2 cells, about 60% of DNA was fragmented at the Exatecan (DX-8951) concentration of 20 ng/ml. Exatecan (DX-8951)(0.05 µg/ml, 24 h ) induced the specific features of apoptosis, namely chromatin condensation, nuclear fragmentation and cytoplasmic vacuolation were apparent in SUIT-2 cells [3].
Exatecan (DX-8951) has shown activity in vivo against a wide range of human tumor xenografts in nude mice, including gastric, pancreatic, colon, breast, ovary, and lung tumors [4]. Exatecan (DX-8951) suppressed the growth of human gastric adenocarcinoma SC-6 xenografted into nude mice. When mice were treated i.v. with Exatecan (DX-8951) three times at 4-day intervals, significant inhibition of tumor growth was observed over a wide dose range (3.325 mg/kg to 50 mg/kg of total dose) without toxic death. Its antitumor activity was dependent on the total dose, and at the highest dose of 50 mg/kg, the tumor growth inhibition rate was 92% [2].
References:
[1]. Kumazawa E, Jimbo T, Ochi Y, et al. Potent and broad antitumor effects of DX-8951f, a water-soluble camptothecin derivative, against various human tumors xenografted in nude mice[J]. Cancer chemotherapy and pharmacology, 1998, 42(3): 210-220.
[2]. Mitsui I, Kumazawa E, Hirota Y, Aonuma M, Sugimori M, Ohsuki S, Uoto K, Ejima A, Terasawa H, Sato K. A new water‐soluble camptothecin derivative, DX‐8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Japanese journal of cancer research. 1995 Aug;86(8):776-82.
[3]. Takiguchi S, Kumazawa E, Shimazoe T, Tohgo A, Kono A. Antitumor effect of DX‐8951, a novel camptothecin analog, on human pancreatic tumor cells and their CPT‐11‐resistant variants cultured in vitro and xenografted into nude mice. Japanese journal of cancer research. 1997 Aug;88(8):760-9.
[4]. De Jager R, Cheverton P, Tamanoi K, et al. DX‐8951f: summary of Phase I clinical trials[J]. Annals of the New York Academy of Sciences, 2000, 922(1): 260-273.
| Cell experiment [1]: | |
Cell lines | 32 malignant cell lines |
Preparation Method | Thus 500-20,000 cells/well in 150 u1 of medium were plated in 96-well flat-bottomed microplates and grown for 24h (P388, CCRF-CEM and K562 cells for 4h), the Exatecan (DX-8951) (in 50 µl medium/well), or the medium alone as a control was added, and the cells were cultured for an additional 3 days. Then calculated Growth inhibition of 50% (GI50) . |
Reaction Conditions | Different concentrations for 24 h |
Applications | Exatecan (DX-8951) showed strong antiproliferating activity,and the mean GI50 values against breast cancers colon cancers, stomach cancers, and lung cancers were 2.02 ng/ml, 2.92 ng/ml, 1.53 ng/ml, and 0.877 ng/ml respectively. |
| Animal experiment [2]: | |
Animal models | Male 6-week-old BALB/c-nu/nu nude mice |
Preparation Method | The human tumor lines inoculated s.c. into nude mice and maintained as solid tumors. Various human tumors maintained in nude mice were excised and |
Dosage form | 50 mg/kg, i.v. |
Applications | The q4d×4 schedule more readily caused the regressive effects of Exatecan (DX-8951) compared with the q7d×3, and a schedule of q4d×3 more frequently permitted regrowth of tumors than did the q4d×4 schedule. |
References: | |
| Cas No. | 171335-80-1 | SDF | |
| Canonical SMILES | O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O | ||
| Formula | C24H22FN3O4 | M.Wt | 435.45 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2965 mL | 11.4824 mL | 22.9647 mL |
| 5 mM | 0.4593 mL | 2.2965 mL | 4.5929 mL |
| 10 mM | 0.2296 mL | 1.1482 mL | 2.2965 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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