XRP44X
Based on 1 Customer Validation
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 729605-21-4
- Formula: C21H21ClN4O
- Molecular Weight:380.87
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Ras 10 nM (IC50) |
XRP44X is an indirect inhibitor of Net phosphorylation that acts upstream from Erk-1/2 activation. XRP44X inhibits luciferase activity with the IC50 of～10 nM[1].
XRP44X (10 nM) inhibits cell growth of HUVEC, NIH3T3, HCT-116, and NIH3T3–Ki-Ras cells[1].
XRP44X (100 nM) inhibits phosphorylation of Mek-1/2 and Raf-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC, NIH3T3, HCT-116, and NIH3T3-Ki-Ras cells
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Concentration:10 nM
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Incubation Time:24, 48, 72, 96 hours
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Result:Inhibited HUVEC, HCT 116,NIH3T3, and NIH3T3-RAS cells proliferation with IC50s of 2.2±0.5 nM, 2.3±0.5 nM, 4±0.5 nM, and 2.3±0.5 nM, respectively.
Inhibited the growth of immortalized mouse fibroblasts.
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Cell Line:HUVEC cells
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Concentration:100 nM
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Incubation Time:Pretreated for 90 minutes
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Result:Inhibited phosphorylation of Rsk-1.
Inhibited phosphorylation of Erk-1/2 on sites required for its activation without affecting overall levels of Erk-1/2.
XRP44X, an inhibitor of Ras/Erk activation of the transcription factor Elk3, inhibits tumor growth and metastasis in mice. XRP44X inhibits tumor growth and metastasis in nude mice. XRP44X decreases the growth of tumours and the formation of metastases in nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude mice (BALB/c nu/nu)[2]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; treated daily for 6 days
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Result:Inhibited cell tumor formation by xenografts in nude mice.
Chemical Information
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CAS No. 729605-21-4
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Appearance Solid
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Molecular Weight 380.87
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Formula C21H21ClN4O
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Color White to off-white
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SMILES
O=C(N1CCN(C2=CC(Cl)=CC=C2)CC1)C3=CC(C)=NN3C4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (131.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Christine Wasylyk, et al. Inhibition of the Ras-Net (Elk-3) pathway by a novel pyrazole that affects microtubules. Cancer Res. 2008 Mar 1;68(5):1275-83. [Content Brief]
[2]. Kostyantyn Semenchenko, et al. XRP44X, an Inhibitor of Ras/Erk Activation of the Transcription Factor Elk3, Inhibits Tumour Growth and Metastasis in Mice. PLoS One. 2016 Jul 18;11(7):e0159531. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6256 mL | 13.1278 mL | 26.2557 mL | 65.6392 mL |
| 5 mM | 0.5251 mL | 2.6256 mL | 5.2511 mL | 13.1278 mL | |
| 10 mM | 0.2626 mL | 1.3128 mL | 2.6256 mL | 6.5639 mL | |
| 15 mM | 0.1750 mL | 0.8752 mL | 1.7504 mL | 4.3759 mL | |
| 20 mM | 0.1313 mL | 0.6564 mL | 1.3128 mL | 3.2820 mL | |
| 25 mM | 0.1050 mL | 0.5251 mL | 1.0502 mL | 2.6256 mL | |
| 30 mM | 0.0875 mL | 0.4376 mL | 0.8752 mL | 2.1880 mL | |
| 40 mM | 0.0656 mL | 0.3282 mL | 0.6564 mL | 1.6410 mL | |
| 50 mM | 0.0525 mL | 0.2626 mL | 0.5251 mL | 1.3128 mL | |
| 60 mM | 0.0438 mL | 0.2188 mL | 0.4376 mL | 1.0940 mL | |
| 80 mM | 0.0328 mL | 0.1641 mL | 0.3282 mL | 0.8205 mL | |
| 100 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6564 mL |
XRP44X Related Classifications
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