AZD3463

AZD3463

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Cited by 1 publications：

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Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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Cited by 1 publications：

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Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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Cited by 1 publications：

Quality Control & MSDS

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Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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PLoS One,2015, 10(11):e0142704

PubMed: 26571493

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Cat.No.	Product Name	Solubility (25°C)
S1068	Crizotinib (PF-02341066)	<1 mg/mL	9 mg/mL	<1 mg/mL
S1108	TAE684 (NVP-TAE684)	<1 mg/mL	3 mg/mL	<1 mg/mL
S2762	Alectinib (CH5424802)	<1 mg/mL	0.5 mg/mL	<1 mg/mL
S7083	Ceritinib (LDK378)	<1 mg/mL	20 mg/mL	3 mg/mL
S7000	AP26113	<1 mg/mL	45 mg/mL	106 mg/mL
S2703	GSK1838705A	<1 mg/mL	107 mg/mL	<1 mg/mL
S7106	AZD3463	<1 mg/mL	24 mg/mL	<1 mg/mL
S8054	ASP3026	<1 mg/mL	14 mg/mL	<1 mg/mL
S7536	PF-06463922	<1 mg/mL	81 mg/mL	30 mg/mL
S7998	Entrectinib (RXDX-101)	<1 mg/mL	100 mg/mL	100 mg/mL

Biological Activity Chemical Information FAQ Tech Support

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse K_m(3)	= 11.2 mg/kg
	rat K_m(6)

1

[1] 104th AACR meeting, 2013, Abst 919.

Download AZD3463 SDF

Molecular Weight (MW)	448.95
Formula	C₂₄H₂₅ClN₆O
CAS No.	1356962-20-3

Storage	3 years -20℃powder
Storage	6 months-80℃in solvent
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	24 mg/mL (53.45 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2-Pyrimidinamine, N-[4-(4-amino-1-piperidinyl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)-

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Ceritinib (LDK378)
Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.

Features:Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
AP26113
AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.

Features:At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.
Alectinib (CH5424802)
Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
ASP3026
ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
ABT-737
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
MGCD-265
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

* Indicates a Required Field

PF-06463922
PF-06463922 is a potent, dual ALK/ROS1 inhibitor with K_i of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. Phase 1.
Erlotinib
Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
R428 (BGB324)
R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
TAE684 (NVP-TAE684)
TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR.
GSK1838705A
GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.

Features:A small-molecule kinase inhibitor of IGF-1R and the insulin receptor.
Alectinib (CH5424802)
Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
AP26113
AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.

Features:At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.
ASP3026
ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
Ceritinib (LDK378)
Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.

Features:Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
Gefitinib (ZD1839)
Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

Features:A potent EGFR tyrosine kinase inhibitor.

Description

AZD3463 is a novel orally bioavailable ALK inhibitor with K_i of 0.75 nM, which also inhibits IGF1R with equivalent potency.

0.75 nM(Ki)

In vitro

AZD3463 is potent in ALK-driven preclinical models and in a variety of crizotinib-resistant models. AZD3463 inhibits ALK in cells as demonstrated by its ability to decrease ALK autophosphorylation in tumor cell lines containing ALK fusions including DEL (ALCL NPM-ALK), H3122 (NSCLC EML4-ALK) and H2228 (NSCLC EML4-ALK). Inhibition of ALK is associated with perturbations in downstream signaling including ERK, AKT and STAT3 pathways leading to preferential inhibition of proliferation in the ALK fusion containing cell lines in vitro. AZD3463 retains good activity against a number of clinically relevant crizotinib resistant mutations including the gatekeeper mutant L1196M where equivalent potency to wild type ALK is observed in vitro and in vivo in EML4-ALK containing BAF3 cell lines. To further assess the potential ability of AZD3463 to overcome additional resistance mechanisms, antiproliferative activity is assessed in multiple crizotinib resistant cell lines independently derived in vitro from H3122 cells as well as a patient derived crizotinib relapsed model. These resistant cell lines contain multiple resistance mechanisms including the L1196M gatekeeper and T115Ins mutations, ALK amplification and/or secondary drivers including EGFR and IGF1R. AZD3463 retains antiproliferative potency within 4 fold of parental H3122 cells for 10 out of 12 of these acquired resistance models in vitro. ^[1]

AZD3463 also demonstrates the ability to dose dependently inhibit pALK in xenograft tumors in vivo resulting in stasis (H3122) or regression (DEL, H2228). ^[1]