NVP-TAE684 5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine
TAE684 (NVP-TAE684)
CAS: 761439-42-3
Molecular Formula: C30H40ClN7O3S
NVP-TAE684 5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine - Names and Identifiers
NVP-TAE684 5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine - Physico-chemical Properties
| Molecular Formula | C30H40ClN7O3S |
| Molar Mass | 614.2 |
| Density | 1.296 |
| Melting Point | 166-169°C |
| Boling Point | 791.0±70.0 °C(Predicted) |
| Solubility | DMSO 3 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Appearance | Solid |
| Color | White to Pale Yellow |
| pKa | 8.14±0.42(Predicted) |
| Storage Condition | Refrigerator, under inert atmosphere |
| Use | TAE684 (NVP-TAE684) is an effective and selective ALK inhibitor with an IC50 of 3 nM, which is 100 times more selective on ALK than on InsR. |
| In vitro study | NVP-TAE684 selectively and effectively inhibit ALK kinase, but there is no obvious cross reaction to other kinases. NVP-TAE684 effectively inhibited Ba/F3 NPM-ALK cell proliferation with an IC50 of 3 nM, and 1 μm NVP-TAE684 had no effect on Ba/F3 cell survival. NVP-TAE684 also inhibited proliferation of NPM-ALK expressing human ALCL cell lines, including Karpas-299 and SU-DHL-1, with an IC50 of 2-5 nM. Molecular models showed that L258 may be one of the main factors affecting the kinase selectivity of NVP-TAE684. Treatment with NVP-TAE684 inhibited phosphorylation by NPM-ALK rapidly and durably. NVP-TAE684 acts on Ba/F3 cells and ALCL patient cell lines expressing NPM-ALK, induces apoptosis, and stops the cell cycle at G1 phase. NVP-TAE684 acts on H3122 CR cells, significantly overcomes the properties of cellular anti-Crizotinib, contains fusion oncogene EML4-ALK, reduces cell growth, inhibits ALK phosphorylation and induces apoptosis. 30 nM NVP-TAE684 can inhibit the expression of mALK R1279Q mutation induced neurite outgrowth. NVP-TAE684 selectively and effectively inhibited ALK kinase, but there was no significant cross-reaction with other kinases. NVP-TAE684 effectively inhibited Ba/F3 NPM-ALK cell proliferation with an IC50 of 3 nM, and 1 μm NVP-TAE684 had no effect on Ba/F3 cell survival. NVP-TAE684 also inhibited proliferation of NPM-ALK expressing human ALCL cell lines, including Karpas-299 and SU-DHL-1, with an IC50 of 2-5 nM. Molecular models showed that L258 may be one of the main factors affecting the kinase selectivity of NVP-TAE684. Treatment with NVP-TAE684 inhibited phosphorylation by NPM-ALK rapidly and durably. NVP-TAE684 acts on Ba/F3 cells and ALCL patient cell lines expressing NPM-ALK, induces apoptosis, and stops the cell cycle at G1 phase. NVP-TAE684 acts on H3122 CR cells, significantly overcomes the properties of cellular anti-Crizotinib, contains fusion oncogene EML4-ALK, reduces cell growth, inhibits ALK phosphorylation and induces apoptosis. 30 nM NVP-TAE684 can inhibit the expression of mALK R1279Q mutation induced neurite outgrowth. |
| In vivo study | After 4 weeks of 3 and 10 mg/kg NVP-TAE684 treatment, the growth and metastasis of the lymphoma were significantly slowed down, and there was no toxicity in the Karpas-299 lymphoma model. Treatment of NVP-TAE684 lymphoma with Karpas-299 also induced disease regression and down-regulation of CD30 expression. NVP-TAE684 effect on H3122 CR transplanted tumor showed obvious anticancer activity. Treatment with NVP-TAE684 also elevated the phenotype of the ALK mutation, especially ALKR1275Q, whereas Crizotinib had no effect on the phenotype. after 4 weeks of treatment with 3 and 10 mg/kg NVP-TAE684, the growth and metastasis of lymphoma were significantly slowed down, and there was no toxicity in the Karpas-299 lymphoma model. Treatment of NVP-TAE684 lymphoma with Karpas-299 also induced disease regression and down-regulation of CD30 expression. NVP-TAE684 effect on H3122 CR transplanted tumor showed obvious anticancer activity. Treatment with NVP-TAE684 also elevated the phenotype of the ALK mutation, especially ALKR1275Q, whereas Crizotinib had no effect on the phenotype. |
NVP-TAE684 5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.628 ml | 8.141 ml | 16.281 ml |
| 5 mM | 0.326 ml | 1.628 ml | 3.256 ml |
| 10 mM | 0.163 ml | 0.814 ml | 1.628 ml |
| 5 mM | 0.033 ml | 0.163 ml | 0.326 ml |
Last Update：2024-01-02 23:10:35
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Product Name: TAE 684 Visit Supplier Webpage Request for quotationCAS: 761439-42-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: TAE684 (NVP-TAE684) Visit Supplier Webpage Request for quotation
CAS: 761439-42-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 761439-42-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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