TAK-632
Based on 5 publication(s) in Google Scholar
TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
For research use only. We do not sell to patients.
- Purity: 98.93%
- CAS No.: 1228591-30-7
- Formula: C27H18F4N4O3S
- Molecular Weight:554.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) TAK-632
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WB
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WB
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WB
All Aurora Kinase Isoforms
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
66 nM
Compound: 8B, TAK-632
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Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
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[PMID: 23906342] |
| A-375 | IC50 |
12 nM
Compound: 8B, TAK-632
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Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis
Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis
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[PMID: 23906342] |
| A-375 | IC50 |
16 nM
Compound: 8B, TAK-632
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Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis
Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis
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[PMID: 23906342] |
| A-375 | IC50 |
160 nM
Compound: 127; TAK-632
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Antiproliferative activity against human A-375 cells harbouring B-Raf V600E mutant by SRB assay
Antiproliferative activity against human A-375 cells harbouring B-Raf V600E mutant by SRB assay
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[PMID: 32798788] |
| A549 | IC50 |
8.5 μM
Compound: TAK-632
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Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTS assay
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[PMID: 26745854] |
| CHL-1 | IC50 |
2.07 nM
Compound: 127; TAK-632
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Antiproliferative activity against human CHL-1 cells harbouring wild type B-Raf by SRB assay
Antiproliferative activity against human CHL-1 cells harbouring wild type B-Raf by SRB assay
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[PMID: 32798788] |
| COLO 205 | IC50 |
0.025 μM
Compound: 3; TAK-632
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Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 27155899] |
| HCT-116 | IC50 |
0.362 μM
Compound: 3; TAK-632
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Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 27155899] |
| HMCB cell line | IC50 |
350 nM
Compound: 127; TAK-632
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Antiproliferative activity against human HMCB cells harbouring wild type B-Raf by SRB assay
Antiproliferative activity against human HMCB cells harbouring wild type B-Raf by SRB assay
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[PMID: 32798788] |
| HMV-2 cell line | GI50 |
200 nM
Compound: 8B, TAK-632
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Antiproliferative activity against human HMVII cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
Antiproliferative activity against human HMVII cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
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[PMID: 23906342] |
| HMV-2 cell line | IC50 |
200 nM
Compound: 127; TAK-632
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Antiproliferative activity against human HMV-2 cells harbouring B-Raf G469V mutant by SRB assay
Antiproliferative activity against human HMV-2 cells harbouring B-Raf G469V mutant by SRB assay
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[PMID: 32798788] |
| HT-144 | IC50 |
110 nM
Compound: 127; TAK-632
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Antiproliferative activity against human HT-144 cells harbouring B-Raf V600E mutant by SRB assay
Antiproliferative activity against human HT-144 cells harbouring B-Raf V600E mutant by SRB assay
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[PMID: 32798788] |
| HT-29 | CC50 |
>50 μM
Compound: 6; TAK-632
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Cytotoxicity against human HT-29 cells measured after 12 hrs by CellTiter-Glo Luminescent assay
Cytotoxicity against human HT-29 cells measured after 12 hrs by CellTiter-Glo Luminescent assay
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[PMID: 31095385] |
| HT-29 | CC50 |
>50 μM
Compound: TAK-632
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Cytotoxicity against human HT-29 cells incubated for 16 to 24 hrs measured by cell-titre glo luminescent cell viability assay
Cytotoxicity against human HT-29 cells incubated for 16 to 24 hrs measured by cell-titre glo luminescent cell viability assay
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[PMID: 36908007] |
| HT-29 | EC50 |
1.44 μM
Compound: 6; TAK-632
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of NFalpha/SM-164/Z-VAD-fmk-induced necroptosis measured after 12 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of NFalpha/SM-164/Z-VAD-fmk-induced necroptosis measured after 12 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 31095385] |
| HT-29 | EC50 |
1.44 μM
Compound: TAK-632; 75
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Anti-necrotic activity in TSZ induced human HT-29 cells incubated for 16 hrs in presence of TSZ by flow cytometry analysis
Anti-necrotic activity in TSZ induced human HT-29 cells incubated for 16 hrs in presence of TSZ by flow cytometry analysis
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[PMID: 36346971] |
| HT-29 | EC50 |
1440 nM
Compound: TAK-632
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TCZ)-induced necroptosis pretreated for 8 to 12 hrs
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TCZ)-induced necroptosis pretreated for 8 to 12 hrs
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[PMID: 33964444] |
| HT-29 | EC50 |
1440 nM
Compound: TAK-632
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of human TNFalpha/Smac mimetic/Z-VAD-FMK induced necroptosis preincubated with compound for 16 hrs followed by TSZ stimulation for 16 hrs by cell-titre glo luminescent cell viability as
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of human TNFalpha/Smac mimetic/Z-VAD-FMK induced necroptosis preincubated with compound for 16 hrs followed by TSZ stimulation for 16 hrs by cell-titre glo luminescent cell viability as
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[PMID: 36908007] |
| HT-29 | EC50 |
1440 nM
Compound: TAK-632
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Anti-necroptic activity in TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis in human HT-29 cells assessed as increase in cell viability preincubated for 30 mins pretreated followed by TSZ stimulation and measured after 16 hrs by MTT assay
Anti-necroptic activity in TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis in human HT-29 cells assessed as increase in cell viability preincubated for 30 mins pretreated followed by TSZ stimulation and measured after 16 hrs by MTT assay
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[PMID: 37917221] |
| HT-29 | IC50 |
0.033 μM
Compound: 3; TAK-632
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Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 27155899] |
| HT-29 | IC50 |
75 nM
Compound: 8B, TAK-632
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Inhibition of BRAF V600E mutant in human HT-29 cells assessed as phosphorylation of MEK
Inhibition of BRAF V600E mutant in human HT-29 cells assessed as phosphorylation of MEK
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[PMID: 23906342] |
| Malme-3M | IC50 |
50 nM
Compound: 127; TAK-632
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Antiproliferative activity against human Malme-3M cells harbouring B-Raf V600E mutant by SRB assay
Antiproliferative activity against human Malme-3M cells harbouring B-Raf V600E mutant by SRB assay
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[PMID: 32798788] |
| SK-MEL-2 | IC50 |
60 nM
Compound: 127; TAK-632
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Antiproliferative activity against human SK-MEL-2 cells harbouring wild type B-Raf by SRB assay
Antiproliferative activity against human SK-MEL-2 cells harbouring wild type B-Raf by SRB assay
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[PMID: 32798788] |
TAK-632 inhibits PDGFRβ, FGFR3, GSK3β, CDK2, P38α, PDGFRα, TIE2, and CDK1 with a range of IC50 values from 120-790 nM. CHK1, IKKβ, and MEK1 are inhibited over an IC50 range of 1400-1700 nM. With 1 h of preincubation time, TAK-632 inhibits BRAF and CRAF in an ATP competitive manner (at low ATP concentrations BRAF IC50: 15 nM; CRAF: 8.1 nM). The respective biochemical activity of TAK-632 against BRAF and CRAF reduces to IC50 values of 58 nM and 62 nM at high ATP concentrations.TAK-632 demonstrates strong inhibition of pMEK and pERK in HMVII cells with IC50 values of 49 nM and 50 nM, respectively[1]. TAK-632 shows strong antiproliferative effects both in A375 and SK-MEL-2 cells (GI50 of 40-190 nM in A375 cells and GI50 of 190-250 nM in SK-MEL-2 cells)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1228591-30-7
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Appearance Solid
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Molecular Weight 554.52
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Formula C27H18F4N4O3S
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Color White to off-white
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SMILES
O=C(NC1=CC(OC2=CC=C3N=C(NC(C4CC4)=O)SC3=C2C#N)=CC=C1F)CC5=CC=CC(C(F)(F)F)=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro. [Abstract]2025 May 8;16(1):4288. PMID: 40341069 -
Br J Pharmacol
Identification of the Raf kinase inhibitor TAK-632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3. [Abstract]2019 Jun;176(12):2095-2108. PMID: 30825190
TAK-632 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108. [Abstract]
HT-29 cells are pretreated with TAK-632 (10 μM) followed by stimulation with TSZ at the indicated time points. Cells are lysed and immunoblotted with the indicated antibodies.
TAK-632 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108. [Abstract]
L929 cells are pretreated with TAK-632 (5 μM) followed by stimulated with mTNF-α (20 ng) plus z-VAD-FMK (20 μM) (TZ) at the indicated time points. Cells are lysed and immunoblotted with the indicated antibodies.
TAK-632 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108. [Abstract]
HEK293T cells are transfected with FLAG-RIPK1 or RIPK3-V5. After 12 h, the cells are treated with TAK-632 as the indicated concentrations for 6 h. Cell lysates are then analyzed by SDS-PAGE and immunoblotted with the indicated antibodies. All western data are representative of five independent experiments.
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Cancer Res Commun
2024 Sep 1;4(9):2454-2462. PMID: 39212544 -
Front Biosci (Landmark Ed)
Hypoxic Regulation of Notch1 Promotes Mitochondrial Fission and Scleral Remodeling in Myopia. [Abstract]2026 Apr 9;31(4):49381. PMID: 42052847 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Solvent & Solubility
DMSO : 100 mg/mL (180.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.51 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Immunoprecipitated BRAF or CRAF is incubated with recombinant inactive MEK (K97R) at 30°C for 30 minutes in kinase reaction buffer containing ATP/Mg2+. RAS/RAF wild-type (A431, CsFb, and HeLa), KRAS-mutant (A549, HCT-116, and MIA PaCa-2), and NRAS-mutant melanoma (GAK, HMV-II, and SK-MEL-2) cells are treated with TAK-632 (0, 0.32, 1.6, 8, 40, 200, 1000 and 5000 nM) at the indicated concentrations for 2 hours. Cell lysates are analyzed by Western blot analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell viability is assessed (3 replicates) using the Sulforhodamine B assay or by the CellTiter-Glo luminescent cell viability assay. The concentrations of TAK-632 that produced 50% growth inhibition (GI50) are calculated using PCP software. The combination index (CI) is calculated using CalcuSyn software. To investigate the antiproliferative activity of TAK-632, we performed proliferation assays in various cell lines harboring mutated BRAF, NRAS, or KRAS. HMV-II, SK-MEL-2, or A375 cells are cotreated with TAK-632 and TAK-733 at the indicated concentrations for 72 hours. Cell viability is measured. The CI value at EC50 is calculated. A375 cells stably expressing NRASQ61K or ΔN-BRAF are cotreated with TAK-632 and TAK-733 at the indicated concentrations for 72 hours. Cell viability is measured. The CI value at EC50 is calculated[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
The xenograft-implanted nude mice are used. Mice bearing SK-MEL-2 xenografts are treated once daily for 21 consecutive days with vehicle or TAK-632 at the indicated concentrations (10 mice per each treatment group). Day 0 indicates the beginning of treatment. Tumors are measured twice a week. Mice bearing SK-MEL-2 xenografts are treated once daily (QD) for 3 days with vehicle, TAK-632 at 60 mg/kg (60 mpk), or TAK-632 at 120 mg/kg (120 mpk). Tumor xenografts are obtained at indicated time points after the final treatment and analyzed by Western blot analysis. Individual blots with dividing lines are combined from a single electrophoresis gel. Bars represent densitometric analysis of phospho-ERK, normalized to vehicle-treated control (mean±SD).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Okaniwa M, et al. Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J Med Chem. 2013 Aug 22;56(16):6478-94. [Content Brief]
[2]. Nakamura A, et al. Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res. 2013 Oct 11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8034 mL | 9.0168 mL | 18.0336 mL | 45.0840 mL |
| 5 mM | 0.3607 mL | 1.8034 mL | 3.6067 mL | 9.0168 mL | |
| 10 mM | 0.1803 mL | 0.9017 mL | 1.8034 mL | 4.5084 mL | |
| 15 mM | 0.1202 mL | 0.6011 mL | 1.2022 mL | 3.0056 mL | |
| 20 mM | 0.0902 mL | 0.4508 mL | 0.9017 mL | 2.2542 mL | |
| 25 mM | 0.0721 mL | 0.3607 mL | 0.7213 mL | 1.8034 mL | |
| 30 mM | 0.0601 mL | 0.3006 mL | 0.6011 mL | 1.5028 mL | |
| 40 mM | 0.0451 mL | 0.2254 mL | 0.4508 mL | 1.1271 mL | |
| 50 mM | 0.0361 mL | 0.1803 mL | 0.3607 mL | 0.9017 mL | |
| 60 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7514 mL | |
| 80 mM | 0.0225 mL | 0.1127 mL | 0.2254 mL | 0.5636 mL | |
| 100 mM | 0.0180 mL | 0.0902 mL | 0.1803 mL | 0.4508 mL |