SCH 51344 (Synonyms: Ras/Rac Transformaton Blocker) |
Catalog No.GC17613
One-Click Copy Product Info
|
SCH 51344 inhibits Ras induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 171927-40-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Kd: 49 nM
SCH 51344 is a potent MTH1 inhibitor.
MTH1, also known as NUDT1, is a nucleotide pool sanitizing enzyme. Loss-of-function of MTH1 impaired growth of KRAS tumour cells. RAS possessed interaction with multiple targets in the cell and regulates at least two signaling pathways, one controlling extracellular signal-regulated kinase (ERK) activation and the other regulating membrane ruffling formation. These two pathways could synergistically cause transformation.
In vitro: SCH 51344 inhibits Ras-accelerated malignant transformation and increases α-actin promoter-stimulated CAT activity in Ras-transformed cells. SCH 51344 has quite little effect on Ras-induced ERK and JNK activation. SCH 51344 inhibits Ras-accelerated membrane ruffling in REF-52 fibroblasts and abolishes anchorage-independent growth of Ras-mediated tumor cell lines. SCH 51344 also induces DNA damage in SW480 colon cancer cells [1,2].
SCH 51344 specifically inhibits membrane ruffling stimulated by activated forms of H-RAS, K-RAS, N-RAS, and RAC. Fibroblast cells treated with this compound had very little effect on activation of ERK and JUN kinase activities mediated by RAS. SCH 51344 was an effective inhibitor of the anchorage-independent growth of Rat-2 fibroblast cells (transformed by the three forms of oncogenic RAS and RAC V12). These facts suggest that a critical component inhibited by SCH 51344 existed in the membrane ruffling pathway downstream from RAC and indicated that this may be an effective approach targeting this pathway to inhibiting transformation by RAS and other oncogenes [1,2].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Walsh AB, Dhanasekaran M, Bar-Sagi D, Kumar CC. SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway. Oncogene. 1997 Nov 20;15(21):2553-60.
[2]. Kumar CC, Ohashi K, Nagata K, Walsh A, Bar-Sagi D, Mizuno K. SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. Ann N Y Acad Sci. 1999; 886: 122-31.
| Cas No. | 171927-40-5 | SDF | |
| Synonyms | Ras/Rac Transformaton Blocker | ||
| Chemical Name | |||
| Canonical SMILES | CC1=NN=C(N2)C1=C(NCCOCCO)C3=C2C=CC(OC)=C3 | ||
| Formula | C16H20N4O3 | M.Wt | 316.35 |
| Solubility | ≥ 31.6mg/mL 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 | 3.1611 mL | 15.8053 mL | 31.6106 mL |
| 5 mM | 632.2 μL | 3.1611 mL | 6.3221 mL |
| 10 mM | 316.1 μL | 1.5805 mL | 3.1611 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 29 reference(s) in Google Scholar.)