Determine the necessary mass, volume, or concentration for preparing a solution.
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SKU | Size | Availability | Price | Qty |
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T129819-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $103.90 | |
T129819-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $155.90 | |
T129819-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $416.90 |
Highly potent, selective ALK inhibitor
Synonyms | 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-pyperidinyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-Pyrimidinediamine | 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine | AB08754 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | TAE684 selectively inhibits the phosphorylation of NPM-ALK, inducing apoptosis and G1 phase arrest in Ba/F3 cell lines. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of ALK receptor tyrosine kinase |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | TAE684 is a potent and selective ALK inhibitor with IC50 of 3 nM, 100-fold more sensitive for ALK than InsR. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine |
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INCHI | InChI=1S/C30H40ClN7O3S/c1-21(2)42(39,40)28-8-6-5-7-26(28)33-29-24(31)20-32-30(35-29)34-25-10-9-23(19-27(25)41-4)37-13-11-22(12-14-37)38-17-15-36(3)16-18-38/h5-10,19-22H,11-18H2,1-4H3,(H2,32,33,34,35) |
InChi Key | QQWUGDVOUVUTOY-UHFFFAOYSA-N |
Canonical SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC |
Isomeric SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC |
PubChem CID | 16038120 |
Molecular Weight | 614.2 |
CAS Registry No. | 761439-42-3 |
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DiscoveRx TREEspot | TAE-684| |
PubChem CID | 16038120 |
ChEMBL Ligand | CHEMBL509032 |
RCSB PDB Ligand | GUI |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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E1528004 | Certificate of Analysis | Jan 15, 2023 | T129819 |
Solubility | DMSO 3 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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1. Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J et al.. (2007) Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.. Proc Natl Acad Sci USA, 104 (1): (270-5). [PMID:17185414] [10.1021/op500134e] |
2. Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.. J Med Chem, 56 (14): (5675-90). [PMID:23742252] [10.1021/op500134e] |
3. Nagashima M et al.. (2020) Midkine-a Is Required for Cell Cycle Progression of Müller Glia during Neuronal Regeneration in the Vertebrate Retina.. J Neurosci, 40 (6): (1232-1247). [PMID:31882403] |