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Brigatinib (AP26113)

Name: Brigatinib (AP26113)
Brand: Selleck Chemicals
SKU: S8229
Rating: 5 (23 reviews)

Catalog No.S8229

For research use only.

Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

CAS No. 1197953-54-0

Selleck's Brigatinib (AP26113) has been cited by 23 publications

Purity & Quality Control

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ALK Signaling Pathway Map

Biological Activity

Description

Targets

ALK ^[1] (Cell-free assay)	ROS1 ^[1] (Cell-free assay)	FLT3 ^[1] (Cell-free assay)	IGF1R ^[1] (Cell-free assay)	EGFR(C797S/del19) ^[2] (cell-based)	Click to View More Targets
0.37 nM	1.9 nM	2.1 nM	24.9 nM	39.9 nM	Click to View More Targets

In vitro

Beyond ALK, IGF1R, and InsR, brigatinib also potently inhibits FLT3 and ROS1 with IC50 values of 2.1 and 1.9 nM, respectively. It does not show significant activity toward c-Met or Ron up to 1 μM^[1]. Brigatinib overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR^[2].

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

KARPAS299	M173R2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		MoTGO\|IhcHK\|	NFzleGtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFHMT{1xd3OrdHn2[UBMSVKSQWOyPVkh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIhQTZiYYH1[Y92eyCxbnWgd49tfXSrb36gZ4VtdCCycn;sbYZmemG2aX;uJIF{e2G7LDDHTVUxKD1iMD6wNUDPxE1w	MnvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzNES4N\|EoRjJ5MUS0PFMyRC:jPh?=
KARPAS299	MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MUe3NkBpenN?	NYHKPHZRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBUGsueG:\|aYTpeoUhU0GUUFHTNlk6KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzKDl4IHHxeYVwfXNib37lJJNwdHW2aX;uJINmdGxicILvcIln\XKjdHnvckBie3OjeTygTWM2OCB;IECuNFI6KM7:TT6=	NFe0R2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0OFg{OSd-MkexOFQ5OzF:L3G+
Ba/F3	NHfLcZJHfW6ldHnvckBie3OjeR?=		NH[3eGM4OiCqcoO=	NVn6W4RXUW6qaXLpeIlwdiCxZjDoeY1idiCHR1\SJIRmdDF7L2S3PVBON0N5OUfTJI12fGGwdDDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhT0l3MDC9JFAvODZ5MjFOwG0v	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF\|NkS2OUc,OjlzM{[0OlU9N2F-
BAF3	NXHyd\|VuSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MnnvO\|IhcHK\|	NEfEN5VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGVITlJiMUnEM3Q4QTCPL1O3PVdUKG23dHHueEBi\nSncjC3NkBpenNiYomgdoV{[Xq3cnnuJIR6\SCkYYPl[EBie3OjeTygTWM2OCB;IECuNlYh\|ryPLh?=	M1rtb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEK5PVU3Lz5\|MESyPVk2PjxxYU6=
BAF3	MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MYS3NkBpenN?	M{LFbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDoZZJjd3KrbnegSWdHWiCOOEW4Vk9VPzlyTT;DO\|k4WyCvdYThcpQh[W[2ZYKgO\|IhcHK\|IHL5JJJme2G8dYLpckBlgWViYnHz[YQh[XO\|YYmsJGlEPTBiPTCwMlQzKM7:TT6=	MmjYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVYoRjNyNEK5PVU3RC:jPh?=
NCI-H1975	NXvFe2UzSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MorBO\|IhcHK\|	MoTYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCQQ1mtTFE6PzViY3XscJMhcGG{Yn;ybY5oKEWJRmKgUFg2QFJxVEe5NG0hdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDy[ZNignW{aX6g[JlmKGKjc3XkJIF{e2G7LDDJR\|UxKD1iMT6wPUDPxE1w	MlPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVYoRjNyNEK5PVU3RC:jPh?=
U937	M{CxSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NGCySVc4OiCqcoO=	M1nVZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVzLMY5m\2G2aY\lJHU6OzdiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJiOU[gZZF2\W:3czDvcoUhe2:udYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKGG\|c3H5MEBKSzVyIE2gN{4yQTRizszNMi=>	NGC1bWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0OFg{OSd-MkexOFQ5OzF:L3G+
KARPAS299	M4PmdmFvfGm2dX3vdkBie3OjeR?=	MkOyOVAhdWdxa3e=	Ml\LNVMh\GG7cx?=	MXLBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh\XiycnXzd4lv\yCQTWCtRWxMKG[3c3nvckBxem:2ZXnuJJhmdm:pcnHmeIVlKGmwIGPDTWQw[mWrZ3WgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEA2OCCvZz;r[{wheG9iYXTtbY5qe3SncnXkJI9v[2ViZHHpcJkh\m:{IEGzJIRigXNuIF7VUGwhRSCQVVzMJO69VS5?	M2j3U\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUS0PFMyLz5{N{G0OFg{OTxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	pEGFR / EGFR / pAkt / Akt / pERK / ERK / pS6 / S6 ; pALK / ALK ; pROS1 / ROS1 / pSTAT3 / STAT3	28287083 21502504 25351743
Growth inhibition assay	Cell viability	25351743

In vivo

Mouse PK parameters for Brigatinib following oral dosing (10 mg/kg): C_max=448 ng/mL,t_1/2=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t_1/2=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, t_max=4 h, t_1/2=3.4 h， F%=52. Brigatinib demonstrates dose-dependent antitumor activity^[1]. Brigatinib demonstrates growth inhibition activity in PC9 triple-mutant xenograft model and in combination with anti-EGFR antibody to potentiate the efficacy both in vitro and in vivo as shown in first-generation EGFR-TKI-resistant patients^[2].

Protocol (from reference)

Cell Research: ^[1]	Cell lines: U937 cells, Karpas-299 cells, H3122 cells Concentrations: -- Incubation Time: 72 h Method: All cell lines were used within 20 passages of the initial thaw. Following inhibitor treatment for 72 h, cell growth was assessed to determine the concentration that causes 50% inhibition of cell viability (IC50).
Animal Research: ^[1]	Animal Models: female CD rats Dosages: 10 mg/kg(p.o); 2 mg/kg(i.v) Administration: p.o, i.v

References

Solubility (25°C)

In vitro	Ethanol	43 mg/mL warmed (73.61 mM)
	DMSO	1 mg/mL warmed (1.71 mM)
	Water	Insoluble

Chemical Information

Molecular Weight	584.09
Formula	C₂₉H₃₉ClN₇O₂P
CAS No.	1197953-54-0
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1CCN(CC1)C2CCN(CC2)C3=CC(=C(C=C3)NC4=NC=C(C(=N4)NC5=CC=CC=C5P(=O)(C)C)Cl)OC

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04925609	Not yet recruiting	Drug: Brigatinib	Anaplastic Large Cell Lymphoma ALK-Positive\|Inflammatory Myofibroblastic Tumor\|Other Solid Tumor	Princess Maxima Center for Pediatric Oncology\|Takeda	December 2021	Phase 1\|Phase 2
NCT04718012	Completed	--	Lung Cancer ROS Translocated	Centre Hospitalier Intercommunal Creteil	March 17 2021	--
NCT04634110	Recruiting	Drug: Brigatinib	Brain Metastases\|Lung Cancer	University of Colorado Denver\|National Cancer Institute (NCI)	November 17 2020	Phase 2
NCT04260009	Withdrawn	Drug: Brigatinib\|Drug: Brigatinib AAF	Anaplastic Lymphoma Kinase Positive (ALK +) Anaplastic Large Cell Lymphoma\|Inflammatory Myofibroblastic Tumors\|Solid Tumors	Takeda	September 1 2020	Phase 1\|Phase 2
NCT04111705	Recruiting	Drug: Lorlatinib	Non Small Cell Lung Cancer Metastatic	Intergroupe Francophone de Cancerologie Thoracique	August 5 2020	Phase 2
NCT04005144	Recruiting	Drug: Binimetinib\|Drug: Brigatinib	ALK Gene Rearrangement\|Lung Non-Small Cell Carcinoma\|Progressive Disease\|ROS1 Gene Rearrangement\|Stage IIIB Lung Cancer\|Stage IIIC Lung Cancer\|Stage IV Lung Cancer\|Stage IVA Lung Cancer\|Stage IVB Lung Cancer	University of California San Francisco\|Takeda\|Array BioPharma	February 25 2020	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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