TAK-632
- Product Name
- TAK-632
- CAS No.
- 1228591-30-7
- Chemical Name
- TAK-632
- Synonyms
- CS-854;TAK-632;TAK-0632;TAK-632, >=98%;4-Tetraglucose;TAK 632; TAK632;TAK-632 USP/EP/BP;TAK632 (Free base);TAK2 63 (Free base);N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)
- CBNumber
- CB52668801
- Molecular Formula
- C27H18F4N4O3S
- Formula Weight
- 554.52
- MOL File
- 1228591-30-7.mol
TAK-632 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 16285
- Product name
- TAK-632
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 16285
- Product name
- TAK-632
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 16285
- Product name
- TAK-632
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
- Product number
- 16285
- Product name
- TAK-632
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $759
- Updated
- 2024/03/01
- Product number
- T004870
- Product name
- TAK632
- Packaging
- 25mg
- Price
- $250
- Updated
- 2021/12/16
TAK-632 Chemical Properties,Usage,Production
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].
target
B-Raf
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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View Lastest Price from TAK-632 manufacturers
- Product
- TAK-632 1228591-30-7
- Price
- US $5.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 1ton
- Release date
- 2019-09-03