MPC-3100 |
Catalog No.GC14322
One-Click Copy Product Info
|
An inhibitor of Hsp90
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 958025-66-6
Sample solution is provided at 25 µL, 10mM.
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MPC-3100 is a purine-based inhibitor of Hsp90 with IC50 value of 60nM [1].
MPC-3100 targets the N-terminal ATP-binding site of Hsp90 and blocks the activity of ATPase. In the Her2-luciferase degradation assay, MPC-3100 reduces this client protein of Hsp90 with IC50 value of 60nM. In HCT-116 cell lines, MPC-3100 inhibits cell proliferation with IC50 value of 540nM. Besides that, MPC-3100 shows a broad spectrum anti-proliferative activity against various cancer cell lines, such as NCI-N87 and DU-145. MPC-3100 also inhibits tumor growth in the NCI-N87 gastric cancer xenograft mode. Moreover, PK studies show that MPC-3100 displays a superior oral PK profile, good overall exposure and a reasonable hepatic clearance rate. Phase I clinical studies demonstrate MPC-3100 is safe and tolerated when administered at doses below 600 mg per day [1].
References:
[1] Kim SH, Bajji A, Tangallapally R, Markovitz B, Trovato R, Shenderovich M, Baichwal V, Bartel P, Cimbora D, McKinnon R, Robinson R, Papac D, Wettstein D, Carlson R, Yager KM. Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor. J Med Chem. 2012 Sep 13;55(17):7480-501.
| Cas No. | 958025-66-6 | SDF | |
| Chemical Name | (2S)-1-[4-[2-[6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]purin-9-yl]ethyl]piperidin-1-yl]-2-hydroxypropan-1-one | ||
| Canonical SMILES | CC(C(=O)N1CCC(CC1)CCN2C3=C(C(=NC=N3)N)N=C2SC4=C(C=C5C(=C4)OCO5)Br)O | ||
| Formula | C22H25BrN6O4S | M.Wt | 549.4 |
| Solubility | Soluble in DMSO | 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 | 1.8202 mL | 9.1008 mL | 18.2017 mL |
| 5 mM | 364 μL | 1.8202 mL | 3.6403 mL |
| 10 mM | 182 μL | 910.1 μL | 1.8202 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)