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Alectinib CAS NO.1256580-46-7
- Min.Order: 1 Gram
- Payment Terms: T/T,MoneyGram,Other
- Product Details
Keywords
- Alectinib
- 1256580-46-7
- 99% purity
Quick Details
- ProName: Alectinib
- CasNo: 1256580-46-7
- Molecular Formula: C30H34N4O2
- Appearance: powder
- Application: intermediate
- DeliveryTime: in stock
- PackAge: According to the need of packing
- Port: Shanghai
- ProductionCapacity: 100 Kilogram/Month
- Purity: 99% purity
- Storage: Sealed in dry,Room Temperature
- Transportation: air,sea,courier
- LimitNum: 1 Gram
- Grade: Industrial Grade,Pharma Grade,Electron...
Superiority
Product Name: Alectinib
Synonyms: AF-802;CH-5424802/RG-7853;Alectinib (CH5424802);AF 802; AF-802; AF802; CH5424802; CH5424802; CH 5424802; RO5424802; RO 5424802; RO5424802, ALECTINIB; BRAND NAME: ALECENSA;brand name: Alecensa;RO 5424802;RO5424802;RO5424802, Alectinib
CAS: 1256580-46-7
MF: C30H34N4O2
MW: 482.62
EINECS: 821-541-6
Product Categories: Anti-cancer&immunity;Inhibitors;API;API
Mol File: 1256580-46-7.mol
Details
Boiling point 722.5±60.0 °C(Predicted)
density 1.28
pka 13.70±0.40(Predicted)
Bioactivity Alectinib (CH5424802) is an efficient ALK inhibitor. Its IC50 is 1.9nM and it is sensitive to the L1196M mutant, which is highly selective for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
Solubility In vitro (25 ° C): DMSO-2 mg/mL heating (4.14 mM); Water-<1 mg/mL (<1 mM); Ethanol-<1 mg/mL (<1 mM)
In vivo (25 ° C): 30% PEG 400/0.5% Tween 80/5% propylene glycol-30 mg/mL.
In vitro Alteinib (CH5424802) can act on ALK and it is ATP-competitive, with a dissociation constant (KD) of 2.4 nM. CH5424802 has a strong inhibitory effect on ALK and L1196M. The Ki is 0.83 and 1.56 nM, respectively. CH5424802 acts on NCI-H2228 NSCLC cells expressing EML4-ALK, inhibiting ALK autophosphorylation. CH5424802 can also inhibit STAT3 and AKT, rather than ERK1/2 phosphorylation. CH5424802 completely inhibited Tyr705, a phosphorylation site of STAT3. CH5424802 preferentially acted on NCI-H2228 cells expressing EML4-ALK without acting on negative NSCLC cell lines that contains ALK, including monolayer cultured HCC827 cells (deletion of EGFR exon19), A549 cells (KRAS mutations) or NCI-H522 cells (EGFR wild type, KRAS wild type, and ALK wild type). CH5424802 acted on NCI-H2228 spherocytes, causing apoptosis-caspase-3/7-like activation. CH5424802 cam inhibit the growth of two lymphoma cells, KARPAS-299 and SR, containing NPM-ALK fusion protein and does not affect the growth of HDLM-2 lymphoma cells without ALK fusion. CH5424802 acted on KARPAS-299 with highly targeted selectivity and stronger antiproliferative activity. When CH5424802 inhibits KAPRAS-299, the IC50 is 3 nM. When inhibit KDR, IC50 was 1.4 μM. The metabolic stability of CH5424802 was high.