PF-06380101 (Synonyms: Aur0101; Auristatin-0101) |
| رقم الكتالوجGC33136 |
PF-06380101 (Aur0101) ، مثبط لأنابيب الأوريستاتين ، هو نظير Dolastatin 10 السام للخلايايُظهر PF-06380101 (Aur0101) فاعلية ممتازة في فحوصات تكاثر الخلايا السرطانية وخصائص ADME التفاضلية عند مقارنتها بنظائر الأوريستاتين الاصطناعية الأخرى المستخدمة في تحضير ADCs
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Cas No.: 1436391-86-4
Sample solution is provided at 25 µL, 10mM.
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PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
[1]. Maderna A, et al. Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications. J Med Chem. 2014 Dec 26;57(24):10527-43.
| Cas No. | 1436391-86-4 | SDF | |
| المرادفات | Aur0101; Auristatin-0101 | ||
| Canonical SMILES | CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C2=NC=CS2)CC3=CC=CC=C3)=O)OC)=O)OC)N(C([C@H](C(C)C)NC(C(C)(C)N)=O)=O)C | ||
| Formula | C39H62N6O6S | M.Wt | 743.01 |
| الذوبان | DMSO : ≥ 65 mg/mL (87.48 mM) | Storage | Store at -20°C |
| 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3459 mL | 6.7294 mL | 13.4588 mL |
| 5 mM | 0.2692 mL | 1.3459 mL | 2.6918 mL |
| 10 mM | 0.1346 mL | 0.6729 mL | 1.3459 mL |
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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.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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