Alectinib Hydrochloride
- Product Name
- Alectinib Hydrochloride
- CAS No.
- 1256589-74-8
- Chemical Name
- Alectinib Hydrochloride
- Synonyms
- Alectinib HCl;Alectinib Hydrochloride;CH-5428402;CPD0098(HCl);CH5424802 HCl;CH-5428402 HCl;Alectinib HCl salt;AF-802 Hydrochloride;RG-7853 Hydrochloride;CH5424802 Hydrochloride
- CBNumber
- CB02570369
- Molecular Formula
- C30H35ClN4O2
- Formula Weight
- 519.09
- MOL File
- 1256589-74-8.mol
Alectinib Hydrochloride Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:3.5(Max Conc. mg/mL);6.74(Max Conc. mM)
- form
- Solid
- color
- White to Off-White
- Stability:
- Hygroscopic
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H341Suspected of causing genetic defects
H361Suspected of damaging fertility or the unborn child
H373May cause damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P281Use personal protective equipment as required.
P308+P313IF exposed or concerned: Get medical advice/attention.
P314Get medical advice/attention if you feel unwell.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- C183365
- Product name
- CH5424802(Alectinib)Hydrochloride
- Packaging
- 10mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- C183365
- Product name
- CH5424802(Alectinib)Hydrochloride
- Packaging
- 50mg
- Price
- $325
- Updated
- 2021/12/16
- Product number
- FA64934
- Product name
- Alectinib hydrochloride
- Packaging
- 50mg
- Price
- $332.5
- Updated
- 2021/12/16
- Product number
- KIN0001508
- Product name
- CH-5424802 HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $503.15
- Updated
- 2021/12/16
- Product number
- SYN5763
- Product name
- AlectinibHydrochloride
- Packaging
- 50mg
- Price
- $547
- Updated
- 2021/12/16
Alectinib Hydrochloride Chemical Properties,Usage,Production
Description
Alectinib hydrochloride, developed by Chugai Pharmaceutical/ Hoffman-La Roche under the trade name Alecensa®, was approved in Japan in April 2014 for the treatment of anaplastic lymphoma kinase (ALK) fusion-gene positive, unresectable, advanced, or recurrent non-small cell lung cancer (NSCLC). The compound is a highly selective second-generation ALK inhibitor, and while alectinib currently remains a focus of further development in Europe and the U.S., the compound has been granted orphan drug designation in Japan after showing a 93.5% objective response rate in phase II clinical trials. In addition to providing rapid treatment response time in a majority of patients, trials showed a 76% 2-year progression-free survival rate. Since the initial approval of crizotinib—the first ALK inhibitor indicated for treatment of ALKrearranged NSCLC —patients treated with crizotinib have shown remarkable improvement as compared to treatment with other chemotherapeutic methods,21 although drug resistance has shown to be a major side effect of this therapy. Preliminary preclinical and clinical studies of alectinib have shown significant promise for overcoming drug resistance developed with other ALK inhibitors.
Uses
CH5424802 Hydrochloride is a highly selective and potent anaplastic lymphoma kinase (ALK) inhibitor capable of blocking the resistant gatekeeper mutant, which results in reduced cell growth. Also is an intermediate of Alectinib (C183360), a highly selective and potent anaplastic lymphoma kinase (ALK) inhibitor capable of blocking the resistant gatekeeper mutant, which results in reduced cell growth.
Definition
ChEBI: Alectinib hydrochloride is a hydrochloride obtained by combining alectinib with one molar equivalent of hydrochloric acid. Used for the treatment of patients with anaplastic lymphoma kinase-positive, metastatic non-small cell lung cancer. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It contains an alectinib(1+).
Synthesis
The synthetic route to alectinib as reported by Chugai begins with 7-methoxy-2-tetralone (1). Bis-methylation with tetrabutylammonium hydrogen sulfide (TBAHS)/aq KOH/MeI followed by bromination with N-bromosuccinimide (NBS) provided the bromo-tetralone 2 in 67% yield over the two steps. Further reaction of 2 with 3-hydrazinobenzonitrile/trifluoroacetic acid (TFA) led to formation of the desired Fischer indole product, albeit as a 1:1 mixture of regioisomers (3/4), which were carried forward as a mixture to oxidation with 2,3-dichloro-5,6-dicyano- 1,4-benzoquinone (DDQ). It is important to note that although representative procedures are published describing the conversion of 2 to alectinib (I), no yields were provided for these transformations. Following oxidation, the desired product 5 could be isolated as a single isomer via precipitation from the crude reaction mixture. Installation of the 4-morpholino-piperidine moiety took place in three transformations from 5, beginning with 1-dodecanethiol/ N-methyl-2-pyrrolidone (NMP)/NaOMe-facilitated methyl cleavage. The corresponding phenol was then readily converted to the triflate intermediate and displaced with 4-(piperidin-4-yl)morpholine (6) at elevated temperature, providing intermediate 7. Crosscoupling of the bromide 7 with ethynyl triisopropylsilane under Pd-catalyzed cross-coupling conditions (Pd(CH3CN)2Cl2/2-dicyclohexylphosphino- 20,40,60-triisopropylbiphenyl (XPhos), reflux) followed by cleavage of the resulting alkylsilane with tetrabutylammonium fluoride (TBAF) yielded the ethynyl precursor to alectinib. Hydrogenation of this unsaturated system under standard conditions (H2, Pd/C) followed by HCl salt formation furnished the final drug target alectinib hydrochloride (I).
IC 50
1.9 nM
Alectinib Hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Alectinib Hydrochloride manufacturers
- Product
- Alectinib hydrochloride (JAN) 1256589-74-8
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100tons
- Release date
- 2023-08-16
- Product
- Alectinib Hydrochloride 1256589-74-8
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 98%
- Supply Ability
- kg
- Release date
- 2023-11-15
- Product
- Alectinib hydrochloride 1256589-74-8
- Price
- US $30.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 1000t/year
- Release date
- 2023-09-07