2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. XRP44X

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.

XRP44X Chemical Structure

XRP44X Chemical Structure

CAS No. : 729605-21-4

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Based on 1 publication(s) in Google Scholar

XRP44X Related Antibodies

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Description

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[1]. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules[2].

IC50 & Target[1]

Ras

10 nM (IC50)

In Vitro

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.

XRP44X Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HUVEC, NIH3T3, HCT-116, and NIH3T3-Ki-Ras cells
Concentration: 10 nM
Incubation Time: 24, 48, 72, 96 hours
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.

Western Blot Analysis[1]

Cell Line: HUVEC cells
Concentration: 100 nM
Incubation Time: Pretreated for 90 minutes
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.
In Vivo

XRP44X may have therapeutic potential for refractory asthma[1].
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.

Animal Model: Male nude mice (BALB/c nu/nu)[2]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; treated daily for 6 days
Result: Inhibited cell tumor formation by xenografts in nude mice.
Molecular Weight

380.87

Formula

C21H21ClN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C2=CC(Cl)=CC=C2)CC1)C3=CC(C)=NN3C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6256 mL 13.1278 mL 26.2557 mL
5 mM 0.5251 mL 2.6256 mL 5.2511 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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XRP44X Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XRP44X729605-21-4RasRas-induced transcriptionRas-Erk-1/2 pathwayrefractory asthmaRas/Erk activationmicrotubulesInhibitorinhibitorinhibit

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