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1256580-46-7

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Product FOB Price Min.Order Supply Ability Supplier
Alectinib 1256580-46-7/50Kg in stock
Cas No: 1256580-46-7
USD $ 10.0-10.0 / Gram 1 Gram 1000 Gram/Day Shenzhen Tianyuan Pharmaceutical Technology Co., Ltd Contact Supplier
alectinib 1256580-46-7
Cas No: 1256580-46-7
USD $ 12.0-12.0 / Gram 100 Gram Metric Ton/Day Wuhan Ying Yuan Bei Biological Limited Contact Supplier
CH5424802 CH-5424802
Cas No: 1256580-46-7
USD $ 3.0-3.0 / Kilogram 1 Kilogram 1-100 Metric Ton/Month Hangzhou Dayangchem Co., Ltd. Contact Supplier
9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
Cas No: 1256580-46-7
No Data 1 Gram 20 Metric Ton/Month Henan Allgreen Chemical Co.,Ltd Contact Supplier
Alectinib
Cas No: 1256580-46-7
No Data No Data No Data Chemwill Asia Co., Ltd. Contact Supplier
Alectinib
Cas No: 1256580-46-7
No Data 500 Gram 500 Kilogram/Month Shanghai Rochi Pharmaceutical Co., Ltd. Contact Supplier
Alectinib CAS: 1256580-46-7
Cas No: 1256580-46-7
USD $ 1.0-2.0 / Metric Ton 5 Metric Ton 1000 Metric Ton/Year Henan Sinotech Import&Export Corporation Contact Supplier
9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
Cas No: 1256580-46-7
No Data 1 Gram 100 Gram/Week HENAN SUNLAKE ENTERPRISE CORPORATION Contact Supplier
high quality 1256580-46-7 Alectinib with best price
Cas No: 1256580-46-7
No Data 10 Gram 1000 Metric Ton/Month Hubei XinRunde Chemical Co., Ltd Contact Supplier
Alectinib
Cas No: 1256580-46-7
USD $ 1.0-1.0 / Metric Ton 1 Metric Ton 1000 Metric Ton/Day Crovell Biotech (Hebei) Co., Ltd. Contact Supplier

1256580-46-7 Usage

Definition

ChEBI: An organic heterotetracyclic compound that is 6,6-dimethyl-5,6-dihydro-11H-benzo[b]carbazol-11-one carrying additional cyano, 4-(morpholin-4-yl)piperidin-1-yl and ethyl substituents at positions 3, 8 and 9 respectively. Used (as the hydr chloride salt) for the treatment of patients with anaplastic lymphoma kinase-positive, metastatic non-small cell lung cancer.

Uses

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.

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.

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.

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.

Chemical Properties

White to Off-White Solid

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.

1256580-46-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile

1.2 Other means of identification

Product number -
Other names Alectinib

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1256580-46-7 SDS

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