Varlitinib
Based on 2 publication(s) in Google Scholar
Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.66%
- CAS. Nr.: 845272-21-1
- Formel: C22H19ClN6O2S
- Molecular Weight:466.94
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Varlitinib
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HER1 7 nM (IC50) |
HER2 2 nM (IC50) |
HER4 4 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1937 | IC50 |
20 μM
Compound: 1
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Anticancer activity against human HCC1937 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human HCC1937 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 33650861] |
| HCC70 | IC50 |
10 μM
Compound: 1
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Anticancer activity against human HCC70 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human HCC70 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 33650861] |
| Hs-578T | IC50 |
10 μM
Compound: 1
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Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 33650861] |
| MDA-MB-453 | IC50 |
0 μM
Compound: 1
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Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 33650861] |
| MDA-MB-468 | IC50 |
0 μM
Compound: 1
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Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 33650861] |
In Vitro
In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib is shown to be highly selective for EGFR/ErbB-2, and does not show any significant activity when screened against a panel of 104 kinases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 845272-21-1
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Appearance Solid
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Molecular Weight 466.94
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Formel C22H19ClN6O2S
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Color Off-white to yellow
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SMILES
C[C@H]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1
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Synonyms
ASLAN001; ARRY-334543
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
Amphiregulin and Epiregulin Confer Radioresistance in Esophageal Squamous Cell Carcinoma Through Oxidative Phosphorylation. [Abstract]2025 Nov 9:e07524. PMID: 41208199
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 33.33 mg/mL (71.38 mM; ultrasonic and warming and heat to 60°C; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.45 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Animal Administration[1]
Mice: The effects of Varlitinib is tested in patient-derived HCC xenograft in SCID mice (HCC29-0909A) with co-expression of HER1, HER2 and HER3 recepors. Mice are treated with Varlitinib when the tumors reach the size of approximately 100-150 mm3. Tumor size measurements are performed twice a week and tumor volumes are calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1416 mL | 10.7080 mL | 21.4160 mL | 53.5401 mL |
| 5 mM | 0.4283 mL | 2.1416 mL | 4.2832 mL | 10.7080 mL | |
| 10 mM | 0.2142 mL | 1.0708 mL | 2.1416 mL | 5.3540 mL | |
| 15 mM | 0.1428 mL | 0.7139 mL | 1.4277 mL | 3.5693 mL | |
| 20 mM | 0.1071 mL | 0.5354 mL | 1.0708 mL | 2.6770 mL | |
| 25 mM | 0.0857 mL | 0.4283 mL | 0.8566 mL | 2.1416 mL | |
| 30 mM | 0.0714 mL | 0.3569 mL | 0.7139 mL | 1.7847 mL | |
| 40 mM | 0.0535 mL | 0.2677 mL | 0.5354 mL | 1.3385 mL | |
| 50 mM | 0.0428 mL | 0.2142 mL | 0.4283 mL | 1.0708 mL | |
| 60 mM | 0.0357 mL | 0.1785 mL | 0.3569 mL | 0.8923 mL |
Varlitinib Related Classifications
HY-10530 Related Classifications
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