N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide
N-[7-cyano-6-[4-fluoro-3-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide
CAS: 1228591-30-7
Molecular Formula: C27H18F4N4O3S
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Names and Identifiers
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Physico-chemical Properties
| Molecular Formula | C27H18F4N4O3S |
| Molar Mass | 554.52 |
| Density | 1.52±0.1 g/cm3(Predicted) |
| pKa | 9.59±0.70(Predicted) |
| Storage Condition | 2-8℃ |
| Physical and Chemical Properties | Bioactive TAK-632 is a potent pan-Raf inhibitor, with IC50 for B- Raf(wt) and C- Raf of 8.3 nM and 1.4 nM, respectively, and poor or no inhibitory effect on other tested enzymes. |
| In vitro study | TAK-632 inhibits phosphorylation of MEK and ERK in the melanoma A375 cell line (BRAF V600E) with an IC50 of 12 nM and 16 nM, respectively. In the human melanoma HMVII cell line (NRAS q61k/BRAFG469V), TAK-632 showed strong inhibition of pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 also had strong antiproliferative activity in A375 and HMVII lines, with GI50 of 66 nM and 200nM, respectively. TAK-632 induces RAF dimerization while slowly inhibiting the kinase activity of RAF due to isolation from RAF. The combination of TAK-632 and TAK-733 exerted synergistic anti-proliferative effects on BRAF-and NRAS-mutated melanoma cells. TAK-632 inhibits phosphorylation of MEK and ERK in melanoma A375 cell line (BRAF V600E) with an IC50 of 12 nM and 16 nM, respectively. In the human melanoma HMVII cell line (NRAS q61k/BRAFG469V), TAK-632 showed strong inhibition of pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 also had strong antiproliferative activity in A375 and HMVII lines, with GI50 of 66 nM and 200nM, respectively. TAK-632 induces RAF dimerization while slowly inhibiting the kinase activity of RAF due to isolation from RAF. The combination of TAK-632 and TAK-733 exerted synergistic anti-proliferative effects on BRAF-and NRAS-mutated melanoma cells. |
| In vivo study | TAK-632 showed excellent oral availability in rats and dogs. TAK-632 (3.9-24.1 mg/kg, p.o.) it exhibited a dose-dependent anti-cancer effect without severe weight loss. In the NRAS-variant melanoma SK-MEL-2 xenograft model, ask -632 (60 or 120 mg/kg, p.o.) also showed potent anti-cancer and no toxicity. TAK-632 showed excellent oral availability in rats and dogs. TAK-632 (3.9-24.1 mg/kg, p.o.) it exhibited a dose-dependent anti-cancer effect without severe weight loss. In the NRAS-variant melanoma SK-MEL-2 xenograft model, ask -632 (60 or 120 mg/kg, p.o.) also showed potent anti-cancer and no toxicity. |
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Upstream Downstream Industry
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.803 ml | 9.017 ml | 18.034 ml |
| 5 mM | 0.361 ml | 1.803 ml | 3.607 ml |
| 10 mM | 0.18 ml | 0.902 ml | 1.803 ml |
| 5 mM | 0.036 ml | 0.18 ml | 0.361 ml |
Last Update：2024-01-02 23:10:35
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Reference Information
| biological activity | TAK-632 is a potent pan-Raf inhibitor for B- Raf(wt) the IC50 values for C- Raf and were 8.3 nM and 1.4 nM, respectively, with little or no inhibition of the other enzymes tested. TAK-632 is a potent pan-Raf inhibitor with an IC50 of 8.3 nM and 1.4 nM for B- Raf(wt) and C- Raf, respectively, in a cell-free assay, inhibition of the other enzymes tested was less effective or had no effect. |
| in vitro study | TAK-632 inhibits phosphorylation of MEK and ERK in melanoma A375 cell line (BRAF V600E), its IC50 was 12 nM and 16 nM, respectively. In the human melanoma HMVII cell line (NRAS q61k/BRAFG469V), TAK-632 showed strong inhibition of pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 also had strong antiproliferative activity in A375 and HMVII lines, with GI50 of 66 nM and 200nM, respectively. TAK-632 induces RAF dimerization while slowly inhibiting the kinase activity of RAF due to isolation from RAF. The combination of TAK-632 and TAK-733 exerted synergistic anti-proliferative effects on BRAF-and NRAS-mutated melanoma cells. TAK-632 inhibits phosphorylation of MEK and ERK in melanoma A375 cell line (BRAF V600E) with an IC50 of 12 nM and 16 nM, respectively. In the human melanoma HMVII cell line (NRAS q61k/BRAFG469V), TAK-632 showed strong inhibition of pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 also had strong antiproliferative activity in A375 and HMVII lines, with GI50 of 66 nM and 200nM, respectively. TAK-632 induces RAF dimerization while slowly inhibiting the kinase activity of RAF due to isolation from RAF. The combination of TAK-632 and TAK-733 exerted synergistic anti-proliferative effects on BRAF-and NRAS-mutated melanoma cells. |
| in vivo study | TAK-632 demonstrated excellent oral availability in mice and dogs. TAK-632 (3.9-24.1 mg/kg, p.o.) it exhibited a dose-dependent anti-cancer effect without severe weight loss. In the NRAS-variant melanoma SK-MEL-2 xenograft model, ask -632 (60 or 120 mg/kg, p.o.) also showed potent anti-cancer and no toxicity. TAK-632 showed excellent oral availability in rats and dogs. TAK-632 (3.9-24.1 mg/kg, p.o.) it exhibited a dose-dependent anti-cancer effect without severe weight loss. In the NRAS-variant melanoma SK-MEL-2 xenograft model, ask -632 (60 or 120 mg/kg, p.o.) also showed potent anti-cancer and no toxicity. |
| features | Orally bioavailable, pan-raf. |
| Target | TargetValue C- Raf (Cell-free assay) 1.4 nM B- Raf (Cell-free assay) 8.3 nM Aurora B (Cell-free assay) 66 nM PDGFR β (Cell-free assay) 120 nM FGFR3 (Cell-free assay) 280 nM |
| Target | Value |
| C-Raf (Cell-free assay) | 1.4 nM |
| B-Raf (Cell-free assay) | 8.3 nM |
| Aurora B (Cell-free assay) | 66 nM |
| PDGFRβ (Cell-free assay) | 120 nM |
| FGFR3 (Cell-free assay) | 280 nM |
Last Update：2024-04-10 22:29:15
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide - Uses and synthesis methods
in vitro studies
TAK-632 inhibits the phosphorylation of MEK and ERK in melanoma A375 cell line (BRAFV600E) with IC50 of 12 nM and 16 nM respectively. In the human melanoma HMVII cell line (NRASQ61K/BRAFG469V), TAK-632 showed strong inhibition to pMEK and pERK with IC50 of 49 nM and 50 nM, respectively. Moreover, TAK-632 has strong antiproliferative activity in A375 and HMVII lines, with GI50 of 66 nM and 200nM respectively. TAK-632 induces RAF dimerization, and at the same time, the kinase activity of RAF is slowly inhibited due to separation from RAF. The combination of TAK-632 and TAK-733 has a synergistic antiproliferative effect on BRAF-and NRAS-mutant melanoma cells.
In vivo studies
TAK-632 showed excellent oral utilization in mice and dogs. When melanoma A375 (BRAFV600E) xenografts and human melanoma HMVII (NRASQ61K/BRAFG469V) xenografts were performed in mice, TAK-632 (3.9-24.1 mg/kg, p.o.) showed a dose-dependent anticancer effect and no severe weight loss. TAK-632 (60 or 120 mg/kg, p.o.) also showed strong anti-cancer and no toxicity in NRAS-heterologous melanoma SK-MEL-2 xenograft model.
features
Orally bioavailable, pan-raf inhibitor that targets both wild-type and mutant forms.
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: TAK 632 Visit Supplier Webpage Request for quotationCAS: 1228591-30-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide
odansetron hydrochloride dihydrate
odansetron hydrochloride dihydrate
Raw Materials for N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide
N-(5-(2-aMino-7-cyanobenzo[d]thiazol-6-yloxy)-2-fluorophenyl)-2-(3-(trifluoroMethyl)phenyl)acetaMide
2-Fluoro-5-nitrobenzonitrile
m-(Trifluoromethyl)phenylacetic acid
3-Amino-4-fluorophenol
Cyclopropanecarbonyl Chloride
2-Fluoro-5-nitrobenzonitrile
m-(Trifluoromethyl)phenylacetic acid
3-Amino-4-fluorophenol
Cyclopropanecarbonyl Chloride