CRA-026440
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- CAS No.: 847460-34-8
- 화학식: C23H24N4O4
- 분자량:420.46
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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HDAC1 4 nM (Ki) |
HDAC8 7 nM (Ki) |
HDAC3 11 nM (Ki) |
HDAC2 14 nM (Ki) |
HDAC6 15 nM (Ki) |
HDAC10 20 nM (Ki) |
CRA-026440 has antiproliferative effect on HUVEC endothelial cells with a GI50 value of 1.41 μM[1].
CRA-026440 (0.1-10 μM; 18 hours) results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis[1].
CRA-026440 (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM
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Incubation Time:18 hours
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Result:Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT-116 tumor-bearing nude mice[1]
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Dosage:100 mg/kg
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Administration:i.v.; daily; for three consecutive days
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Result:Resulted in a statistically significant reduction in tumor growth.
Chemical Information
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CAS No. 847460-34-8
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분자량 420.46
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화학식 C23H24N4O4
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SMILES
O=C(C(N1)=CC2=C1C=CC(OCCN(C)C)=C2)NCC#CC3=CC=C(C(NO)=O)C=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
DMSO : 100 mg/mL (237.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3783 mL | 11.8917 mL | 23.7835 mL | 59.4587 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7567 mL | 11.8917 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3783 mL | 5.9459 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5856 mL | 3.9639 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1892 mL | 2.9729 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9820 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |
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