Alectinib (Synonyms: CH5424802; RO5424802; RG7853)

Name: Alectinib
Brand: MedChemExpress
SKU: HY-13011
Rating: 5.0 (43 reviews)

Cat. No.: HY-13011 Purity: 99.78%: Data Sheet
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Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.

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CAS No. : 1256580-46-7

사이즈	재고	수량
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	해외재고보유	Estimated Time of Arrival: December 31
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고객리뷰

Based on 43 publication(s) in Google Scholar

Other Forms of Alectinib:

43 Publications Citing Use of MCE Alectinib

: Alectinib purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2018 May 10:4:56. [Abstract]; NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.

: Alectinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]; Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.

: Alectinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]; In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively^[1]. Alectinib demonstrates effective central nervous system (CNS) penetration^[2].

IC₅₀ & Target

IC50: 1.9 nM(ALK), 1 nM (ALK^F1174L), 3.5 nM (ALK^R1275Q)^[1]
Kd: 2.4 nM (ALK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 1000 1 Compound: 1	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	>1 3 Compound: 1	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	169 1 Compound: 1	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	3 1 Compound: 1	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: 4; CH5424802	Antiproliferative activity against human KARPAS299 cells Antiproliferative activity against human KARPAS299 cells	[PMID: 31419130]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: 18a, CH5424802	Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay	[PMID: 22225917]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: Alectinib	Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
BaF3	IC₅₀	207 1 Compound: 1	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
SR	IC₅₀	3.4 1 Compound: Alectinib	Antiproliferative activity against ALK positive human SR cells Antiproliferative activity against ALK positive human SR cells	[PMID: 33751979]
BaF3	IC₅₀	3 1 Compound: 1	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NB1	IC₅₀	4.5 1 Compound: Alectinib	Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
BaF3	IC₅₀	169 1 Compound: 1	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	72 1 Compound: 1	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NCI-H2228	IC₅₀	4.5 1 Compound: 4; CH5424802	Inhibition of EML4/ALK in human NCI-H2228 cells Inhibition of EML4/ALK in human NCI-H2228 cells	[PMID: 31419130]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	9 1 Compound: 1	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	90 1 Compound: 1	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NCI-H2228	IC₅₀	6.5 1 Compound: CH5424802	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	15 1 Compound: 3; CH5424802	Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	IC₅₀	9 1 Compound: 1	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 1 Compound: 1	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: Alectinib	Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
BaF3	IC₅₀	2067 1 Compound: Alectinib	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3 Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3	[PMID: 27780853]
NCI-H3122	EC₅₀	9 1 Compound: 1	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: 18a, CH5424802	Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay	[PMID: 22225917]
BaF3	IC₅₀	207 1 Compound: 1	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NCI-H3122	IC₅₀	9 1 Compound: 4; CH5424802	Cytotoxicity against human NCI-H3122 cells Cytotoxicity against human NCI-H3122 cells	[PMID: 31419130]
KARPAS-299	IC₅₀	47 1 Compound: 3	Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
KARPAS-299	IC₅₀	15 1 Compound: 3; CH5424802	Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	IC₅₀	3 1 Compound: 1	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
Kelly	EC₅₀	434 1 Compound: 1	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NCI-H3122	IC₅₀	17.4 1 Compound: 3; CH5424802	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	IC₅₀	72 1 Compound: 1	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	9 1 Compound: 1	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NB1	IC₅₀	4.5 1 Compound: Alectinib	Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H3122	IC₅₀	19 1 Compound: 5	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
NCI-H2228	IC₅₀	53 1 Compound: Alectinib	Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
BaF3	IC₅₀	90 1 Compound: 1	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
SU-DHL-1	IC₅₀	20.5 1 Compound: 3; CH5424802	Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NCI-H2228	IC₅₀	6.5 1 Compound: CH5424802	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
NIH3T3	IC₅₀	32.3 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	IC₅₀	> 1000 1 Compound: 1	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NCI-H3122	IC₅₀	45 1 Compound: 3	Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
BaF3	IC₅₀	> 2000 1 Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
NCI-H3122	IC₅₀	17.4 1 Compound: 3; CH5424802	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NCI-H3122	IC₅₀	19 1 Compound: 5	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
KARPAS-299	IC₅₀	47 1 Compound: 3	Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
BaF3	IC₅₀	> 2000 1 Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
NCI-H3122	IC₅₀	45 1 Compound: 3	Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
NCI-H2228	IC₅₀	53 1 Compound: Alectinib	Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
BaF3	IC₅₀	> 2000 1 Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	72 1 Compound: 1	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NCI-H3122	EC₅₀	9 1 Compound: 1	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
HCC78	IC₅₀	> 1000 1 Compound: CH5424802; AF-802	Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
NIH3T3	IC₅₀	132 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	IC₅₀	90 1 Compound: 1	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
NIH3T3	IC₅₀	132 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NIH3T3	IC₅₀	32.3 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
HCC78	IC₅₀	> 10000 1 Compound: CH5424802; AF-802	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	169 1 Compound: 1	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
SH-SY5Y	EC₅₀	1150 1 Compound: 1	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
BaF3	IC₅₀	207 1 Compound: 1	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
SK-N-AS	EC₅₀	2139 1 Compound: 1	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	2401 1 Compound: 1	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
Kelly	EC₅₀	434 1 Compound: 1	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KARPAS-299	IC₅₀	15 1 Compound: 3; CH5424802	Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
SK-N-SH	EC₅₀	872 1 Compound: 1	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: 18a, CH5424802	Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay	[PMID: 22225917]
SK-N-SH	EC₅₀	872 1 Compound: 1	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SH-SY5Y	EC₅₀	1150 1 Compound: 1	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SU-DHL-1	IC₅₀	20.5 1 Compound: 3; CH5424802	Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
KARPAS-299	IC₅₀	3 1 Compound: 4; CH5424802	Antiproliferative activity against human KARPAS299 cells Antiproliferative activity against human KARPAS299 cells	[PMID: 31419130]
SK-N-AS	EC₅₀	2139 1 Compound: 1	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KARPAS-299	IC₅₀	3 1 Compound: Alectinib	Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
SK-N-FI	EC₅₀	2401 1 Compound: 1	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
KARPAS-299	IC₅₀	47 1 Compound: 3	Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
Kelly	EC₅₀	434 1 Compound: 1	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NB1	IC₅₀	4.5 1 Compound: Alectinib	Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	4.5 1 Compound: 4; CH5424802	Inhibition of EML4/ALK in human NCI-H2228 cells Inhibition of EML4/ALK in human NCI-H2228 cells	[PMID: 31419130]
NCI-H2228	IC₅₀	53 1 Compound: Alectinib	Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	6.5 1 Compound: CH5424802	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
NCI-H3122	EC₅₀	9 1 Compound: 1	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NCI-H3122	IC₅₀	17.4 1 Compound: 3; CH5424802	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NCI-H3122	IC₅₀	19 1 Compound: 5	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
NCI-H3122	IC₅₀	45 1 Compound: 3	Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
NCI-H3122	IC₅₀	9 1 Compound: 4; CH5424802	Cytotoxicity against human NCI-H3122 cells Cytotoxicity against human NCI-H3122 cells	[PMID: 31419130]
NIH3T3	IC₅₀	132 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NIH3T3	IC₅₀	32.3 1 Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
SH-SY5Y	EC₅₀	1150 1 Compound: 1	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-AS	EC₅₀	2139 1 Compound: 1	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	2401 1 Compound: 1	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-SH	EC₅₀	872 1 Compound: 1	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SR	IC₅₀	3.4 1 Compound: Alectinib	Antiproliferative activity against ALK positive human SR cells Antiproliferative activity against ALK positive human SR cells	[PMID: 33751979]
SU-DHL-1	IC₅₀	20.5 1 Compound: 3; CH5424802	Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]

In Vitro

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT^[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 nM,10 nM,100 nM, 1000 nM
Incubation Time:	2 hours
Result:	Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay^[1]

Cell Line:	HCC827, A549, or NCIH522 cells
Concentration:	0-1000 nM
Incubation Time:	5 days
Result:	Reduced cell activity in a dose-dependent manner.

In Vivo

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC₅₀ of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID or nude mice bearing NCI-H2228 cells^[1]
Dosage:	0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:	Oral administration; once daily; for 11 days
Result:	Resulted in dose-dependent tumor growth inhibition (EC₅₀ of 0.46 mg/kg) and tumor regression.

Clinical Trial

분자량

482.62

화학식

C₃₀H₃₄N₄O₂

CAS No.

1256580-46-7

Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6CCOCC6)=C(C=C4C3=O)CC)C)C=C1

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 4.33 mg/mL (8.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0720 mL	10.3601 mL	20.7202 mL
5 mM	0.4144 mL	2.0720 mL	4.1440 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

This protocol yields a clear solution of ≥ 0.38 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

This protocol yields a clear solution of ≥ 0.38 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (25.90 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.78%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (248 KB) HNMR (141 KB) RP-HPLC (247 KB) MS (74 KB)

Handling Instructions (2659 KB)

References

[1]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690. [Content Brief]

[2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0720 mL	10.3601 mL	20.7202 mL	51.8006 mL
DMSO	5 mM	0.4144 mL	2.0720 mL	4.1440 mL	10.3601 mL

Alectinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Alectinib (Synonyms: CH5424802; RO5424802; RG7853)

고객리뷰

Other Forms of Alectinib:

43 Publications Citing Use of MCE Alectinib

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농도 희석 계산기

Complete Stock Solution Preparation Table

Alectinib Related Classifications

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Alectinib (Synonyms: CH5424802; RO5424802; RG7853)

고객리뷰

Other Forms of Alectinib:

Alectinib Related Antibodies

43 Publications Citing Use of MCE Alectinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

순도&문서

References

고객리뷰

Alectinib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Alectinib Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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