PIM1-IN-1 |
| رقم الكتالوجGC65278 |
PIM1-IN-1 هو مثبط PIM1 / 3 قوي وانتقائي للغاية ، مع IC50s من 7 و 5530 و 70 نانومتر لـ PIM1 و PIM2 و PIM3 ، على التوالي ، يمنع فسفرة BAD ، وهو هدف مصب لـ PIM ، مع EC50 262 نانومترلا يظهر PIM1-IN-1 أي تأثير واضح على ربط FLT3 أو hERGنشاط مضاد للتكاثر ومضاد للسرطان
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1417630-95-5
Sample solution is provided at 25 µL, 10mM.
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PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity[1].
PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI50 of 1.48 µM for melanoma cell line SKMEL-19. PIM1-IN-1 has significant synergistic effect combined with different antitumoral agents in different tumor cell lines[1]. PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells[1].
PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice[1].
[1]. MartÍnez-GonzÁlez S, et al. Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem. 2019 Feb 19;168:87-109.
PIM1 7nM(IC50) | PIM3 70nM(IC50) | PIM2 5530nM(IC50) |
| Cas No. | 1417630-95-5 | SDF | |
| Formula | C25H30N8O2 | M.Wt | 474.56 |
| الذوبان | DMSO : 45 mg/mL (94.82 mM; Need ultrasonic) | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1072 mL | 10.5361 mL | 21.0722 mL |
| 5 mM | 421.4 μL | 2.1072 mL | 4.2144 mL |
| 10 mM | 210.7 μL | 1.0536 mL | 2.1072 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
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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