CH5424802
CH5424802 is a potent and selective ALK inhibitor.
Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers. .
In vitro: In cell free assays the IC50 of CH5424802 for enzyme activity of ALK was 1.9 nM; the dissociation constant (KD) value for ALK in an ATP-competitive manner was 2.4 nM. The inhibitory activity for two hot spot-activating mutations (F1174L and R1275Q) in neuroblastoma was comparable to that for wildtype ALK [1].
In vivo: In the NCI-H2228 model, oral administration of CH5424802 resulted in dose-dependent tumor growth inhibition (ED50 = 0.46 mg/kg) and tumor regression. Moreover, treatment of 20 mg/kg CH5424802 showed rapid tumor regression and tumor regrowth did not occur throughout the 4-week drug-free period [2].
Clinical trial: No clinical data are available currently.
Reference:
[1] Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 482.62 |
| Cas No. | 1256580-46-7 |
| Formula | C30H34N4O2 |
| Solubility | insoluble in H2O; ≥2.72 mg/mL in EtOH with gentle warming; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic |
| Chemical Name | 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | CCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | Alectinib (CH5424802) is a potent inhibitor of ALK with an IC50 value of 1.9 nM. | |||||
| Targets | ALK (F1174L) | ALK | ALK (R1275Q) | INSR | KDR | |
| IC50 | 1 nM | 1.9 nM | 3.5 nM | 550 nM | 1.4 μM | |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
