9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile basic information

bioactivity solubility in vitro in vivo

product name:	9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile
synonyms:	9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile;ch5424802;af-802;ch-5424802/rg-7853;alectinib (ch5424802);alectinib;af-802,rg-7853;9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile alectinib (ch5424802)
cas:	1256580-46-7
mf:	c30h34n4o2
mw:	483
einecs:
product categories:	anti-cancer&immunity;inhibitors
mol file:	1256580-46-7.mol

9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile chemical properties

density

1.28

safety information

msds information

9-ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5h-benzo[b]carbazole-3-carbonitrile usage and synthesis

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.
in vivo	the oral treatment of ch5424802 can inhibit tumor growth. this role is dose-dependent, and the ed50 is 0.46 mg/kg. ch5424802 was treated at a dose of 20 mg/kg, causing a rapid regression of the tumor, with a recurrent rate of 168%. after 11 days of treatment (at day 28), the tumor volume in each mouse was less than 30 mm3, maintaining an effective anti-tumor effect; no tumor regurgitation occurs in no drug treatment period whitin 4 weeks.the half-life and oral bioavailability for ch5424802 treated mice were 8.6 hours and 70.8%, respectively. the mean plasma levels were 1.7, 1.5, and 0.3 nm after the treatment of 6 mg/kg repeated doses for 2, 7, and 24 hours.ch5424802 treatment inhibited tumor growth.use ch5424802 to treat karpas-299 and nb-1 at a dose of 20 mg/kg, and on day 20, tumor growth was inhibited by 119% and 104%.ch5424802 inhibited stat3 phosphorylation, which is dose-dependent (2-20 mg/kg), a decrease in phosphorylation of akt was observed in the xenografts treated with ch5424802.
chemical properties	white to off-white solid
usage	ch5424802 is a highly selective and potent anaplastic lymphoma kinase (alk) inhibitor capable of blocking the resistant gatekeeper mutant, which results in reduced cell growth. ch5424802 have been cl inically evaluated for the treatment of patients with alk-driven tumors.

company information

henan sunlake enterprise corporation is located in henan province , the central plain of china , which enjoys favorable geogeaphical position and convenient transportion. the com[any was established in june. 1998, until now having more than 18 years experience in manufacturing & exporting chemical raw material .

sunlake is a professional manufacturer engaged in producing and selling chemicals,including organic & inorganic chemicals , pigments & dyestuffs , water treatment chemicals , food & feed additives and others. these products have been being well exported to europe, southeast asia, the middle east ,africa, south america and some other countries and areas.

we sincerely welcome foreign friends to visit our plant for cooperation. with the idea of "quality first,credit priority, excellent service", we are highly acknowledged by customers for good quality and competitive price. more importantly , the company has a strong r & d team, who are professional engineers and scholars with ph. d. .so we are confident to serve you better with our high - quality products and professional team. we are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional supplier in international market.

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