Dolastatin 10 video
I.Dolastatin 10 basic Characters:
|Storage Temp:||Store in a cool and dry place and at 0 – 4℃ for short term(days to weeks) or -57℃ for long term (months to years)|
|Color:||White to off-white sollid|
II. Dolastatin 10 (110417-88-4) usage in antitumor cycle
Dolastatin 10 (CAS 110417-88-4), Dolastatin-10, Neuro_000215, CCRIS 7310, CID100208, NSC376128,NSC 376128, C11280, L-Valinamide, N,N-dimethyl-L-valyl-N-(2-methoxy-4-(2-(1-methoxy-2-methyl-3-oxo-3-((2-phenyl-1-(2-thiazolyl)ethyl)amino)propyl)-1-pyrrolidinyl)-1-(1-methylpropyl)-4-oxobutyl)-N-methyl-, (2S-(1(1R*(R*),2S*),2R*(1S*,2S*,3(R*))))-
2.Dolastatin 10 Usage:
Purpose: Medical scientist investigated the efficacy and toxicity of the novel anti-microtubule agent dolastatin-10 in patients with advanced breast cancer.
Methods: Twenty-one patients with measurable metastatic breast cancer were treated with dolastatin-10 at a dose of 400 mcg/m2 by intravenous bolus once every 3 weeks.
Results: One out of 21 patients (5%; 95% CI: 0–24%) achieved a partial remission for a duration of 113 days. Four patients maintained stable disease for a median of 87 days. Patients received a median of two cycles of dolastatin-10. Hematologic toxicity was moderate, with 8 patients developing grade 4 neutropenia, and 5 with grade 3 neutropenia; one grade 3 febrile neutropenia was observed. These episodes of grade 3 and 4 neutropenia were experienced on 36% of the treatment cycles. Non-hematologic toxicity was uncommon.
Conclusion: While the toxicity profile of dolastatin-10 was acceptable, it had minimal activity in this advanced breast cancer study.
In Vitro: Dolastatin 10 is a unique pentapeptide that isolated from the sea hare Dolabella auricularia. It is founds that these in vitro data are quite comparable to those of Dolastatin 10 and Auristatin PE, each of which has GI50 values of 10−5-10−6 μg/mL (10−2-10−3 nM) against a similar minipanel of human cell lines. The antibody-drug conjugate (ADC) comprises the anti-CD30 monoclonal antibody cAC10 conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), a synthetic analog of the tubulin polymerization inhibitor Dolastatin 10 (110417-88-4).
3.Warning on Dolastatin 10
This product is for research use only, not for human or veterinary use.
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Dolastatin 10 synthesis
Total synthesis of Dolastatin 10 (110417-88-4) was completed by developing an efficient synthesis of two key amino acid components, Dil (6) and Dap (11), and subsequent stepwise coupling of five amino acid components from C-terminal Doe.
Synthesis and Evaluation of Dolastatin 10 Analogues Containing Heteroatoms on the Amino Acid Side Chains.
Synthetic analogues of the natural occurring dolastatin 10 are of great interest in cancer due to their potent in vitro activity and their uses as payloads in antibody drug conjugates (ADCs). Modification of the dolastatin 10 core scaffold has mainly focused on modifications of the P1, N-terminus, and P5, C-terminus, with minimal attention to the P2 subunit.
In the cellular assay, Dolastatin 10 (110417-88-4) shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as OVCAR-3 and NSCLC) with IC50 values ranging from 0.1nM to 10nM. It is currently tested in the clinical trials.
III. Dolastatin 10 (110417-88-4) HCML
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