| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
CA224 (Compound 1) (48 hours) treatment against human cancer cell lines demonstrated antiproliferative efficacy [1]. CA224 (18–48 hours) selectively destroys SV40 large T antigen-transformed normal mouse embryonic liver cells (BNL S A.8) and inhibits the growth of cancer cells in the G0/G1 and G2/M phases of the cell cycle [1][2]. Tubulin polymerization is inhibited and stable tubulin depolymerization is enhanced by CA224 (0–4 µM, 30 min) [1]. Cancer cells undergo apoptosis when exposed to CA224 (0-72 h) [1]. Inhibiting CYP3A4, CYP2D6, CYP2C9, and CYP2C19 by 50%, 14%, 51%, and 19%, respectively, is the effect of CA224 (10 μM) [1].
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| ln Vivo |
Significant tumor growth inhibition was demonstrated by CA224 (Compound 1) (100 mg/kg; intraperitoneal injection; once daily for 9 days) without overt toxicity [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI-H1299, NCI-H358, BNL CL2 and BNL SV A.8 Tested Concentrations: Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated anti-proliferative activity against LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI- with IC50 values of 3.5, 6.2, 4.0, 3.5, 11.5, 2.0, 2.5, 2.2, 2.6 and 3.8 uM are H1299, NCI-H358, BNL CL2 and BNL SV A.8 respectively. Cell cycle analysis[1][2] Cell Types: A549, NCI-H1299, NCI-H358, BNL CL2, BNL SV A.8 and Calu-1 Tested Concentrations: IC50 concentration (IC70 for Calu-1) Incubation Duration: 24 hrs (hours) 18 hrs (hours) for NCI-H358 and 48 hrs (hours) for BNL CL2 and BNL SV for A549, NCI-H1299 and Calu-1 A.8 Experimental Results: Deep blockade was induced at G2/M in A549 and NCI-H1299 cells. Maintenance of nocodazole- and paclitaxel-induced G2/M arrest in NCI-H358 cells. BNL CL2 cells exhibit significant G2/M phase arrest. In BNL S A.8 cells 31% of cells were detected in sub-G1 phase (control: 0%). G0/G1 blockade is preserved in serum- |
| Animal Protocol |
Animal/Disease Models: Severe combined immunodeficiency (SCID) mice, which lack T and B immune cells. Male mice weighing 18~25 g and 6~8 weeks old were injected subcutaneously (sc) (sc) with HCT-116, and female mice weighing 15~24 g and 6~8 weeks old were injected subcutaneously (sc) (sc) with NCI-H460[1].
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 9 days. Experimental Results: It demonstrated significant tumor growth inhibition in both HCT-116 and NCI-H460 tumor models, and there was no significant decrease in body weight. Animal/Disease Models: balb/c (Bagg ALBino) mouse [1] Doses: 10 mg/kg (oral) or 1.0 mg/kg (iv) Route of Administration: Oral or intravenous (iv) (iv)(pharmacokinetic/PK/PK analysis) Experimental Results: After IV and PO Determination of administrative pharmacokinetic/PK/PK parameters of CA224 [1]. Parameter IV (1 mg/kg) Oral (10 mg/kg) t1/2,β (h) 0.33 1.16 AUC0-t (ng·h/mL) 187 172 AUC0-∞ (ng·h/mL) 189 182 Cmax (ng/mL) 371 190 Vd (L/Kg) 2.52 nd Vdss (L/Kg) 1.76 nd CL (mL/min/kg) 88.3 nd Bioavailability - 9.6% t1/2,β Time point 0.5 consid |
| References |
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| Molecular Formula |
C24H22N2O
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|---|---|
| Molecular Weight |
354.444
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| Exact Mass |
354.173
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| CAS # |
883561-04-4
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| PubChem CID |
11610059
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| Appearance |
White to off-white solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2=C(C=CC=C2)C(CCN(C)C(C2=CC=C(C3=CC=CC=C3)C=C2)=O)=C1
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| InChi Key |
CPKLVRIYXBROSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H22N2O/c1-26(16-15-21-17-25-23-10-6-5-9-22(21)23)24(27)20-13-11-19(12-14-20)18-7-3-2-4-8-18/h2-14,17,25H,15-16H2,1H3
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| Chemical Name |
N-[2-(1H-indol-3-yl)ethyl]-N-methyl-4-phenylbenzamide
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| Synonyms |
CA-224; CA 224; CA224
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~282.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8214 mL | 14.1068 mL | 28.2135 mL | |
| 5 mM | 0.5643 mL | 2.8214 mL | 5.6427 mL | |
| 10 mM | 0.2821 mL | 1.4107 mL | 2.8214 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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