Cat. No.: HY-10192

NVP-TAE 684

(Synonyms: TAE 684)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC₅₀ values between 2 and 10 nM.

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Pureté: 99.70%
CAS No.: 761439-42-3
Formule: C₃₀H₄₀ClN₇O₃S
Masse moléculaire:614.20

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

NVP-TAE 684 Chemical Structure

CAS No.: 761439-42-3

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC₅₀ values between 2 and 10 nM^[1].

IC₅₀ & Target

IC50: 2-10 nM (ALK-dependent cell lines)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.1 μM Compound: 14; TAE684	Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
BaF3	IC₅₀	0.001 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay	[PMID: 21572589]
BaF3	IC₅₀	0.004 μM Compound: TAE-684	Inhibition of Tel-fused ALK kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused ALK kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	0.02 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	IC₅₀	0.06 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	IC₅₀	0.08 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	IC₅₀	0.554 μM Compound: TAE-684	Inhibition of Tel-fused FLT3 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused FLT3 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	0.872 μM Compound: TAE-684	Inhibition of Tel-fused FLT1 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused FLT1 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.048 μM Compound: TAE-684	Inhibition of Tel-fused Abl kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused Abl kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.146 μM Compound: TAE-684	Inhibition of Tel-fused SRC kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused SRC kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.167 μM Compound: TAE-684	Inhibition of Tel-fused Tie2 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused Tie2 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.216 μM Compound: TAE-684	Inhibition of Tel-fused FGFR1 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused FGFR1 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.3 μM Compound: TAE-684	Inhibition of Tel-fused EphB4 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused EphB4 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.308 μM Compound: TAE-684	Inhibition of Tel-fused Lyn kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused Lyn kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.313 μM Compound: TAE-684	Inhibition of Tel-fused KitQ kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused KitQ kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.385 μM Compound: TAE-684	Inhibition of Tel-fused RET kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused RET kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.474 μM Compound: TAE-684	Inhibition of Tel-fused Syk kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused Syk kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.505 μM Compound: TAE-684	Inhibition of Tel-fused JAK2 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused JAK2 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.578 μM Compound: TAE-684	Inhibition of Tel-fused Bmx kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused Bmx kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.598 μM Compound: TAE-684	Inhibition of Tel-fused ZAP70 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused ZAP70 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.634 μM Compound: TAE-684	Inhibition of Tel-fused RON kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused RON kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1.667 μM Compound: TAE-684	Inhibition of Tel-fused MET kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused MET kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	1336 nM Compound: 4, TAE684	Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	IC₅₀	2 nM Compound: TAE684	Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells	[PMID: 25461320]
BaF3	IC₅₀	2.018 μM Compound: TAE-684	Inhibition of Tel-fused TRKB kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused TRKB kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	2.123 μM Compound: TAE-684	Inhibition of Tel-fused KDR kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused KDR kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	2.309 μM Compound: TAE-684	Inhibition of Tel-fused TYK2 kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused TYK2 kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	2.751 μM Compound: TAE-684	Inhibition of mouse wild type BaF3/WT Luc+ cell proliferation Inhibition of mouse wild type BaF3/WT Luc+ cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	229.3 nM Compound: 18; TAE684	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	229.3 nM Compound: 8	Cytotoxicity against mouse BaF3 cells expressing EGFR-Del19/C797S mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR-Del19/C797S mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 36417820]
BaF3	IC₅₀	3 nM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing NPM-ALK after 48 hrs by CellTiter-Glo assay Cytotoxicity against mouse BAF3 cells expressing NPM-ALK after 48 hrs by CellTiter-Glo assay	[PMID: 21572589]
BaF3	IC₅₀	3.22 μM Compound: TAE-684	Inhibition of Tel-fused PDGFRb kinase-mediated mouse BaF3 cell proliferation Inhibition of Tel-fused PDGFRb kinase-mediated mouse BaF3 cell proliferation	[PMID: 17185414]
BaF3	IC₅₀	3.7 nM Compound: 4, TAE684	Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	IC₅₀	340.7 nM Compound: 18; TAE684	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	340.7 nM Compound: 8	Cytotoxicity against mouse BaF3 cells harboring EGFR C797S/T790M/del19 mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells harboring EGFR C797S/T790M/del19 mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo assay	[PMID: 36417820]
BaF3	IC₅₀	43.7 nM Compound: 4, TAE684	Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
HEK293	IC₅₀	21.9 nM Compound: TAE684	Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	6.1 nM Compound: TAE684	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	7.8 nM Compound: TAE684	Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	93.3 nM Compound: TAE684	Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
KARPAS-299	IC₅₀	<10 nM Compound: TAE-684	Decrease in ALK phosphorylation in human Karpas299 cells after 4 hrs Decrease in ALK phosphorylation in human Karpas299 cells after 4 hrs	[PMID: 17185414]
KARPAS-299	IC₅₀	13 nM Compound: 2, NVP-TAE684	Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs	[PMID: 24900831]
KARPAS-299	IC₅₀	14 nM Compound: 7; TAE684	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
KARPAS-299	IC₅₀	2 nM Compound: TAE-684	Antiproliferative activity against human Karpas299 cells assessed as luciferase expression after 72 hrs Antiproliferative activity against human Karpas299 cells assessed as luciferase expression after 72 hrs	[PMID: 17185414]
KARPAS-299	IC₅₀	2.4 nM Compound: 4, TAE684	Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
KARPAS-299	IC₅₀	3 nM Compound: TAE-684	Induction of apoptosis in human Karpas299 cells by annexin V assay Induction of apoptosis in human Karpas299 cells by annexin V assay	[PMID: 17185414]
Kelly	IC₅₀	0.38 μM Compound: 1, TAE684	Cytotoxicity against human Kelly cells expressing ALK F1174L mutant Cytotoxicity against human Kelly cells expressing ALK F1174L mutant	[PMID: 21572589]
NCI-H1975	GI₅₀	0.72 μM Compound: 14; TAE684	Growth inhibition of human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
NCI-H2228	IC₅₀	16 nM Compound: 2; NVP-TAE684	Inhibition of EML4/ALK in human NCI-H2228 cells Inhibition of EML4/ALK in human NCI-H2228 cells	[PMID: 31419130]
NCI-H3122	IC₅₀	44 nM Compound: 2; NVP-TAE684	Inhibition of EML4/ALK in human NCI-H3122 cells Inhibition of EML4/ALK in human NCI-H3122 cells	[PMID: 31419130]
SH-SY5Y	IC₅₀	0.16 μM Compound: 1, TAE684	Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant	[PMID: 21572589]
SU-DHL-1	IC₅₀	2 nM Compound: TAE-684	Antiproliferative activity against human SUDHL1 cells assessed as luciferase expression after 72 hrs Antiproliferative activity against human SUDHL1 cells assessed as luciferase expression after 72 hrs	[PMID: 17185414]

In Vitro

TAE684 inhibits the proliferation of Ba/F3 NPM-ALK cells with an IC₅₀ of 3 nM, without affecting the survival of parental Ba/F3 cells at concentrations up to 1 μM. TAE684 inhibits STAT3 and STAT5 phosphorylation in a dose-dependent manner in both Ba/F3 NPM-ALK and Karpas-299 cells. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines^[1].
NVP-TAE684 markedly reduces cell survival in both sensitive H3122 and H3122 CR cells, but has little to no effect on the viability of other, non-ALK-dependent cancer cell lines. NVP-TAE684 treatment of H3122 CR cells suppresses phosphorylation of ALK, AKT, and ERK and induces marked apoptosis.
TAE684 potently suppresses the survival of Ba/F3 cells expressing the EML4-ALK L1196M mutant^[2].
Neurite outgrowth induced by expression of the mALKR1279Q mutant is completely inhibited at 30 nM NVP-TAE684, which is comparable with the response seen with activated wt mALK^[3].

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

In Vivo

NVP-TAE684 suppresses lymphomagenesis in two independent models of ALK-positive ALCL and induces regression of established Karpas-299 lymphomas. TAE684 displays appreciable bioavailability and half-life in vivo.
TAE684 (1, 3, and 10 mg/kg. p.o.) significantly delays in lymphoma development and shows 100- to 1,000-fold reduction in luminescence signal. The TAE684- (10 mg/kg) treated group appeares healthy and does not display any signs of compound- or disease-related toxicity^[1].

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

Chemical Information

CAS No. 761439-42-3
Appearance Solid
Masse moléculaire 614.20
Formule C₃₀H₄₀ClN₇O₃S
Color Light yellow to yellow
SMILES

O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCC(N5CCN(CC5)C)CC4)C=C3OC)=NC=C2Cl)(C(C)C)=O
Synonyms

TAE 684
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (14)

All In Vivo Efficacy StudyIF

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Journal Impact Factor

Theranostics

Midkine signaling maintains the self-renewal and tumorigenic capacity of glioma initiating cells. [Abstract]

2020 Apr 6;10(11):5120-5136. PMID: 32308772
Cell Death Dis

Fyn inhibition by TAE684: A synergistic strategy to suppress melanoma and reverse vemurafenib resistance. [Abstract]

2025 Nov 6;16(1):796. PMID: 41198656
Cell Chem Biol

Exploring the target scope of KEAP1 E3 ligase-based PROTACs. [Abstract]

2022 Oct 20;29(10):1470-1481.e31. PMID: 36070758
Cell Chem Biol

Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions. [Abstract]

2018 Feb 15;25(2):224-229.e2. PMID: 29276046
Mol Cancer Res

EML4-ALK Variant 3 Promotes Mitotic Errors and Spindle Assembly Checkpoint Deficiency Leading to Increased Microtubule Poison Sensitivity. [Abstract]

2022 Jun 3;20(6):854-866. PMID: 35656694
Pharmaceuticals (Basel)

Therapeutic Implications of Ceritinib in Cholangiocarcinoma beyond ALK Expression and Mutation. [Abstract]

2024 Feb 2;17(2):197. PMID: 38399413
Biomolecules

Lysophosphatidic Acid Stimulates Mitogenic Activity and Signaling in Human Neuroblastoma Cells through a Crosstalk with Anaplastic Lymphoma Kinase. [Abstract]

2024 May 28;14(6):631. PMID: 38927035
BMC Biol

Ontogenetic and phylogenetic simplification during white stripe evolution in clownfishes. [Abstract]

2018 Sep 5;16(1):90. PMID: 30180844
ACS Chem Biol

A simple, highly visual in vivo screen for anaplastic lymphoma kinase inhibitors. [Abstract]

2012 Dec 21;7(12):1968-74. PMID: 22985331

NVP-TAE 684 purchased from MedChemExpress. Usage Cited in: ACS Chem Biol. 2012 Dec 21;7(12):1968-74. [Abstract]

TAE684 inhibits NPM-Ltk. Wild-type embryos are injected with 30 pg of psox10:NPM-Ltk and treated with 3 μM of TAE684. Incident light images at 3 dpf of control uninjected, nontreated embryo (a); NPM-Ltk injected, DMSO-treated sibling (b); and NPM-Ltk injected TAE684-treated siblings (c).
Pigment Cell Melanoma Res

Developmental and comparative transcriptomic identification of iridophore contribution to white barring in clownfish. [Abstract]

2019 May;32(3):391-402. PMID: 30633441
Pigment Cell Melanoma Res

Zebrafish Leucocyte tyrosine kinase controls iridophore establishment, proliferation and survival. [Abstract]

2016 May;29(3):284-96. PMID: 26801003

NVP-TAE 684 purchased from MedChemExpress. Usage Cited in: Pigment Cell Melanoma Res. 2016 May;29(3):284-96. [Abstract]

Ltk inhibitor TAE684 partially rescues the ltk^mne phenotype and decreases the number of iridophores. The number of iridophores is reduced in ltk^mne/+ larvae treated with ALK inhibitor TAE684 from 82 to 105 hpf.
J Gene Med

The CHST11 gene is linked to lung cancer and pulmonary fibrosis. [Abstract]

2022 Sep 30;e3451. PMID: 36181245
Cancer Chemother Pharmacol

Targeting ALK in pediatric RMS does not induce antitumor activity in vivo. [Abstract]

2018 Aug;82(2):251-263. PMID: 29855693
University of Tubingen

2016 Jan.

Solvant et solubilité

In Vitro:

DMSO : 7.69 mg/mL (12.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

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5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6281 mL

8.1407 mL

16.2813 mL

5 mM

0.3256 mL

1.6281 mL

3.2563 mL

10 mM

0.1628 mL

0.8141 mL

1.6281 mL

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.

Calculateur de molarité

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In Vivo:

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

Stock Solution Working Solution

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: ≥ 0.77 mg/mL (1.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.77 mg/mL (1.25 mM); Clear solution

This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, BCR-ABL, or TEL-kinase fusion constructs are plated in 384-well plates (25,000 cells per well) and incubated with serial dilutions of TAE684 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. ICsub>50 values are generated by using XLFit software.

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

Animal Administration^[1]

For in vivo compound efficacy studies, treatment is initiated 72 h after tail vein injection of 1×10⁶ Karpas-299-, Ba/F3 NPM-ALK- or BCR-ABL-expressing cells into female Fox Chase SCIDBeige mice. Mice (n=10 per group) are administered either TAE684 resuspended in 10% 1-methyl-2-pyrrolidinone/90% PEG 300 solution at 1, 3, and 10 mg/kg once daily for 3 weeks or the vehicle solution at the same dosing schedule. Disease progression and compound efficacy is monitored weekly with bioluminescence imaging. To determine the efficacy of TAE684 on established disease, dosing is initiated on day 12, at which time the disease confirmed to be widespread by bioluminescence imaging. For analysis of downstream molecular effects in vivo, mice with established lymphomas are administered vehicle solution or TAE684 (10 mg/kg) for 3 days. At the end of treatment, mice are killed, and lymph nodes are extracted for immunoblotting and histological analysis.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Instruction de manipulation (2659 KB)

Références

[1]. Galkin AV, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. [Content Brief]

[2]. Katayama R, et al. Therapeutic strategies to overcome PF-02341066 resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. [Content Brief]

[3]. Schonherr C, Activating ALK mutations found in neuroblastoma are inhibited by PF-02341066 and NVP-TAE684. Biochem J. 2011 Dec 15;440(3):405-13. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6281 mL	8.1407 mL	16.2813 mL	40.7034 mL
	5 mM	0.3256 mL	1.6281 mL	3.2563 mL	8.1407 mL
	10 mM	0.1628 mL	0.8141 mL	1.6281 mL	4.0703 mL

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NVP-TAE 684

14 Cited Publications

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NVP-TAE 684

Lorlatinib

Ceritinib

Dasatinib

Crizotinib

MS4078

Ruxolitinib

PD173955

Flavopiridol

Mitoxantrone

BAPTA-AM

Maraviroc

Torkinib

Publications Citing Use of MedChemExpress (MCE) NVP-TAE 684

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

NVP-TAE 684

Lorlatinib

Ceritinib

Dasatinib

Crizotinib

MS4078

Ruxolitinib

PD173955

Flavopiridol

Mitoxantrone

BAPTA-AM

Maraviroc

Torkinib

Publications Citing Use of MedChemExpress (MCE) NVP-TAE 684

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

NVP-TAE 684 Related Classifications

HY-10192 Related Classifications

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