Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listTAK-632

TAK-632

  • CAS NO.:1228591-30-7
  • Empirical Formula: C27H18F4N4O3S
  • Molecular Weight: 554.52
  • MDL number: MFCD26960965
  • EINECS: 200-256-5
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-20 11:41:24
TAK-632 Structural

What is TAK-632?

The Uses of TAK-632

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].

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.

Properties of TAK-632

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

Safety information for TAK-632

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for TAK-632

Related products of tetrahydrofuran

You may like

  • N-[7-cyano-6-(4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy)-1,3-benzothiazol-2-yl]cyclopropanecarboxamide 95% CAS 1228591-30-7
    N-[7-cyano-6-(4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy)-1,3-benzothiazol-2-yl]cyclopropanecarboxamide 95% CAS 1228591-30-7
    1228591-30-7
    View Details
  • TAK632 97.20% CAS 1228591-30-7
    TAK632 97.20% CAS 1228591-30-7
    1228591-30-7
    View Details
  • 1823368-42-8 98%
    1823368-42-8 98%
    1823368-42-8
    View Details
  • 2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    1307449-08-6
    View Details
  • Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    25408-95-1
    View Details
  • 2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    1805639-70-6
    View Details
  • 1784294-80-9 98%
    1784294-80-9 98%
    1784294-80-9
    View Details
  • Lithium Clavulanate
    Lithium Clavulanate
    61177-44-4
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.