KRCA-0008
Based on 1 publication(s) in Google Scholar
KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 96.19%
- CAS No.: 1472795-20-2
- Formula: C30H37ClN8O4
- Molecular Weight:609.12
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Publications Citing Use of MedChemExpress (MCE) KRCA-0008
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Biological Activity
IC50: 12 nM (ALK), 4 nM (Ack1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H3122 | IC50 |
0.031 μM
Compound: KRCA-008
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Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell proliferation
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[PMID: 30114660] |
KRCA-0008 (0-1000 μM) shows potency to ALK (wt), ALK L1196 M, ALK C1156Y, ALK F1174L, ALK R1275Q and insulin receptor with IC50s of 12, 75, 4, 17, 17 and 210 nM, respectively[1].? KRCA-0008 (0-1000 nM; 4 h) inhibits ALK-dependent signaling pathways more potently than crizotinib[2].? KRCA-0008 (0-1000 nM; 72 h) induces cell apoptosis[2].? KRCA-0008 (0-100 nM; 48 h) affects cell cycle[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H3122 and H1993 cell lines
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Concentration:200 nM
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Incubation Time:6 hours
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Result:Inhibited cell proliferation of H3122 and H1993 cells with IC50s of 0.08 and 3.6 nM, respectively.
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Cell Line:NPM-ALK-positive ALCL cell lines (Karpas-299 and SU-DHL-1) and U937 NPM ALK-negative lymphoma cell line
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Concentration:200 nM
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Incubation Time:72 hours
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Result:Inhibited proliferation of Karpas-299, SU-DHL-1 and U937 cells with GI50s of 12 nM, 3 nM and 3.5 μM, respectively.
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Cell Line:Karpas-299 and SU-DHL-1 cell lines
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Concentration:0, 10, 100 and 1000 nM
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Incubation Time:4 hours
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Result:Completely suppressed phosphorylation of ALK and its effectors at a dose of 100 nM in NPM-ALK-positive ALCL cells.
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Cell Line:SU-DHL-1 cell line
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Concentration:0-1 μM
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Incubation Time:72 hours
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Result:Dose-dependently increased cspase-3/7 activities and induced cell apoptosis.
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Cell Line:Karpas-299 and SU-DHL-1 cell lines
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Concentration:0-100 nM
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Incubation Time:48 hours
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Result:Induced G0/G1 cell cycle arrest in ALCL cells expressing NPM-ALK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice with Karpas-299 xenografts[2]
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Dosage:25 and 50 mg/kg
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Administration:Oral gavage; 25 and 50 mg/kg twice a day; for two weeks
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Result:Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss.
Chemical Information
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CAS No. 1472795-20-2
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Appearance Solid
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Molecular Weight 609.12
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Formula C30H37ClN8O4
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Color White to gray
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SMILES
ClC1=CN=C(NC2=CC=C(N3CCN(C(C)=O)CC3)C=C2OC)N=C1NC4=CC=C(N5CCN(C(C)=O)CC5)C=C4OC
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Chem Biol Interact
CHMFL-BMX-078, a BMX inhibitor, overcomes the resistance of melanoma to vemurafenib via inhibiting AKT pathway. [Abstract]2022 Jan 5:351:109747. PMID: 34813779
Solvent & Solubility
DMSO : 230 mg/mL (377.59 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution
This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Park CH, et al. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. [Content Brief]
[2]. Hwang J, et al. KRCA-0008 suppresses ALK-positive anaplastic large-cell lymphoma growth. Invest New Drugs. 2020 Oct;38(5):1282-1291. [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 | 1.6417 mL | 8.2086 mL | 16.4171 mL | 41.0428 mL |
| 5 mM | 0.3283 mL | 1.6417 mL | 3.2834 mL | 8.2086 mL | |
| 10 mM | 0.1642 mL | 0.8209 mL | 1.6417 mL | 4.1043 mL | |
| 15 mM | 0.1094 mL | 0.5472 mL | 1.0945 mL | 2.7362 mL | |
| 20 mM | 0.0821 mL | 0.4104 mL | 0.8209 mL | 2.0521 mL | |
| 25 mM | 0.0657 mL | 0.3283 mL | 0.6567 mL | 1.6417 mL | |
| 30 mM | 0.0547 mL | 0.2736 mL | 0.5472 mL | 1.3681 mL | |
| 40 mM | 0.0410 mL | 0.2052 mL | 0.4104 mL | 1.0261 mL | |
| 50 mM | 0.0328 mL | 0.1642 mL | 0.3283 mL | 0.8209 mL | |
| 60 mM | 0.0274 mL | 0.1368 mL | 0.2736 mL | 0.6840 mL | |
| 80 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5130 mL | |
| 100 mM | 0.0164 mL | 0.0821 mL | 0.1642 mL | 0.4104 mL |
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