- TAK-632
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- $35.00 / 5mg
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2025-04-28
- CAS:1228591-30-7
- Min. Order:
- Purity: 98.5%
- Supply Ability: 10g
- TAK-632
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- $5.00 / 5KG
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2019-09-04
- CAS:1228591-30-7
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 1ton
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| | TAK-632 Basic information |
| Product Name: | TAK-632 | | Synonyms: | TAK-632;N-(7-CYANO-6-(4-FLUORO-3-(2-(3-(TRIFLUOROMETHYL)PHENYL)ACETAMIDO)PHENOXY)BENZO[D]THIAZOL-2-YL)CYCLOPROPANECARBOXAMIDE;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide;TAK-0632;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide TAK632;TAK 632 N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide;TAK-632, >=98%;TAK2 63 (Free base) | | CAS: | 1228591-30-7 | | MF: | C27H18F4N4O3S | | MW: | 554.52 | | EINECS: | 200-256-5 | | Product Categories: | Inhibitors | | Mol File: | 1228591-30-7.mol |  |
| | TAK-632 Chemical Properties |
| density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥27.75 mg/mL in DMSO; insoluble in H2O; ≥2.23 mg/mL in EtOH with gentle warming and ultrasonic | | form | solid | | pka | 9.59±0.70(Predicted) | | color | White to off-white |
| | TAK-632 Usage And Synthesis |
| Uses | TAK-632 is a selective pan-RAF inhibitor. It exhibits antitumor activity by inducing RAF dimerization but inhibiting its kinase activity in BRAF- and NRAS-mutated with acquired resistance to BRAF inhibitor in human and mouse melanoma cell. | | Definition | ChEBI: TAK-632 is a member of the class of benzothiazoles that is 1,3-benzothiazole substituted by (cyclopropanecarbonyl)amino, 4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy, and cyano groups at positions 2, 6 and 7, respectively. It is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF(V600E), BRAF(WT), respectively. It has a role as a necroptosis inhibitor, a B-Raf inhibitor, an EC 2.7.11.26 (tau-protein kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of monofluorobenzenes, a member of benzothiazoles, an aromatic ether, a secondary carboxamide, a member of (trifluoromethyl)benzenes, a nitrile and a cyclopropylcarboxamide. | | Biological Activity | tak-632 is a selective inhibitor of braf, craf and braf-v600e kinase with ic50 value of 8.3 nm, 1.4 nm and 2.4 nm [1].raf kinases are a family of three serine/threonine-specific protein kinases and play an important role in the ras-raf-mek-erk signal transduction cascade, as well as the mitogen-activated protein kinase (mapk) cascade [2].tak-632 is a potent pan-raf kinase inhibitor and has a higher selectivity compared with the reported pan-raf kinase inhibitor vemurafenib. when tested with sk-mel-2 cells, tak-632 showed induction on the braf-craf dimmers formation in a dose-dependent manner. in melanoma cell lines a375 and sk-mel-2, tak-632 exhibited significant antiproliferative effects with gi50 value of 6 nom/l and 11 nom/l, respectively [1].in mouse model with sk-mel-2 subcutaneous xenograft, oral administration of tak-632 caused significant reduction of phosphorylated erk and tumor growth at the dose of 60 or 120 mg/kg/d once daily for 21 days without severe toxicity [1].it is also reported that tak-632 is a potent inhibitor of perk with ic50 value of 25 nm [1]. | | in vivo | TAK-632 demonstrates dramatically improved solubility (740 μg/mL) in pH 6.8 phosphate buffer and exhibits significant oral absorption (at a dose of 25 mg/kg, AUC, 32.47 μg h/mL; F, 51.7%) in rats. In a dog PK study, 10 mg/kg administration of TAK-632 also shows superior oral bioavailability (F: 108%).Oral single administration of TAK-632 inhibits pERK in tumors at 8 h after its administration over a dose range of 1.9-24.1 mg/kg. In particular, 9.7-24.1 mg/kg dosing with TAK-632 strongly inhibits pERK levels to 11% of the control. TAK-632 exhibits dose-dependent antitumor efficacy without severe body weight reduction over a dose range of 3.9-24.1 mg/kg. Significant tumor regression is observed at 9.7 mg/kg and 24.1 mg/kg (T/C=?2.1% and ?12.1%, respectively)[1]. TAK-632 exhibits potent antitumor efficacy when orally administered at 60 mg/kg once daily (T/C=37%, P<0.001) or at 120 mg/kg once daily (T/C=29%, P<0.001) for 21 days without severe toxicity in NRAS-mutant melanoma using a SK-MEL-2 xenograft model[2]. | | target | B-Raf | | IC 50 | c-Raf: 1.4 nM (IC50); Braf: 8.3 nM (IC50); Aurora B: 66 nM (IC50); PDGFRβ: 120 nM (IC50); PDGFRα: 610 nM (IC50); FGFR3: 280 nM (IC50); TIE2: 740 nM (IC50); IKKβ: 3700 nM (IC50); CDK1: 790 nM (IC50); CDK2: 580 nM (IC50); p38α: 600 nM (IC50); GSK3β: 500 nM (IC50); MEK1: 3700 nM (IC50) | | references | [1]. nakamura, a., et al., antitumor activity of the selective pan-raf inhibitor tak-632 in braf inhibitor-resistant melanoma. cancer res, 2013. 73(23): p. 7043-55.
[2]. korkut, a., et al., perturbation biology nominates upstream-downstream drug combinations in raf inhibitor resistant melanoma cells. elife, 2015. 4. |
| | TAK-632 Preparation Products And Raw materials |
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