BRAF V600E/CRAF-IN-2
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases.
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- CAS No.: 2499499-62-4
- 화학식: C30H30F3N5O2
- 분자량:549.59
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
3.73 μM
Compound: 9c
|
Growth inhibition of human 786-0 cells measured after 48 hrs by SRB assay
Growth inhibition of human 786-0 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| A498 | GI50 |
4.94 μM
Compound: 9c
|
Growth inhibition of human A498 cells measured after 48 hrs by SRB assay
Growth inhibition of human A498 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| A549 | GI50 |
1.05 μM
Compound: 9c
|
Growth inhibition of human A549 cells measured after 48 hrs by SRB assay
Growth inhibition of human A549 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| ACHN | GI50 |
1.21 μM
Compound: 9c
|
Growth inhibition of human ACHN cells measured after 48 hrs by SRB assay
Growth inhibition of human ACHN cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| BT-549 | GI50 |
3.78 μM
Compound: 9c
|
Growth inhibition of human BT-549 cells measured after 48 hrs by SRB assay
Growth inhibition of human BT-549 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| CAKI-1 | GI50 |
0.917 μM
Compound: 9c
|
Growth inhibition of human CAKI-1 cells measured after 48 hrs by SRB assay
Growth inhibition of human CAKI-1 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| CCRF-CEM | GI50 |
0.758 μM
Compound: 9c
|
Growth inhibition of human CCRF-CEM cells measured after 48 hrs by SRB assay
Growth inhibition of human CCRF-CEM cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| COLO 205 | GI50 |
0.654 μM
Compound: 9c
|
Growth inhibition of human COLO 205 cells measured after 48 hrs by SRB assay
Growth inhibition of human COLO 205 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| DU-145 | GI50 |
1.88 μM
Compound: 9c
|
Growth inhibition of human DU-145 cells measured after 48 hrs by SRB assay
Growth inhibition of human DU-145 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| EKVX | GI50 |
3.07 μM
Compound: 9c
|
Growth inhibition of human EKVX cells measured after 48 hrs by SRB assay
Growth inhibition of human EKVX cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HCC 2998 | GI50 |
0.72 μM
Compound: 9c
|
Growth inhibition of human HCC 2998 cells measured after 48 hrs by SRB assay
Growth inhibition of human HCC 2998 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HCT-116 | GI50 |
0.872 μM
Compound: 9c
|
Growth inhibition of human HCT-116 cells measured after 48 hrs by SRB assay
Growth inhibition of human HCT-116 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HCT-15 | GI50 |
0.798 μM
Compound: 9c
|
Growth inhibition of human HCT-15 cells measured after 48 hrs by SRB assay
Growth inhibition of human HCT-15 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HL-60(TB) | GI50 |
3.82 μM
Compound: 9c
|
Growth inhibition of human HL-60(TB) cells measured after 48 hrs by SRB assay
Growth inhibition of human HL-60(TB) cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HOP-62 | GI50 |
1.02 μM
Compound: 9c
|
Growth inhibition of human HOP-62 cells measured after 48 hrs by SRB assay
Growth inhibition of human HOP-62 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HOP-92 | GI50 |
1.26 μM
Compound: 9c
|
Growth inhibition of human HOP-92 cells measured after 48 hrs by SRB assay
Growth inhibition of human HOP-92 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| Hs-578T | GI50 |
3.61 μM
Compound: 9c
|
Growth inhibition of human Hs-578T cells measured after 48 hrs by SRB assay
Growth inhibition of human Hs-578T cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| HT-29 | GI50 |
0.572 μM
Compound: 9c
|
Growth inhibition of human HT-29 cells measured after 48 hrs by SRB assay
Growth inhibition of human HT-29 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| IGROV-1 | GI50 |
0.924 μM
Compound: 9c
|
Growth inhibition of human IGROV-1 cells measured after 48 hrs by SRB assay
Growth inhibition of human IGROV-1 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| K562 | GI50 |
0.91 μM
Compound: 9c
|
Growth inhibition of human K562 cells measured after 48 hrs by SRB assay
Growth inhibition of human K562 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| KM12 | GI50 |
1.71 μM
Compound: 9c
|
Growth inhibition of human KM12 cells measured after 48 hrs by SRB assay
Growth inhibition of human KM12 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| LOX IMVI | GI50 |
0.78 μM
Compound: 9c
|
Growth inhibition of human LOX IMVI cells measured after 48 hrs by SRB assay
Growth inhibition of human LOX IMVI cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| M14 | GI50 |
0.668 μM
Compound: 9c
|
Growth inhibition of human M14 cells measured after 48 hrs by SRB assay
Growth inhibition of human M14 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| Malme-3M | GI50 |
0.611 μM
Compound: 9c
|
Growth inhibition of human Malme-3M cells measured after 48 hrs by SRB assay
Growth inhibition of human Malme-3M cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| MCF7 | GI50 |
0.679 μM
Compound: 9c
|
Growth inhibition of human MCF7 cells measured after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| MDA-MB-231 | GI50 |
1.8 μM
Compound: 9c
|
Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| MDA-MB-435 | GI50 |
1.16 μM
Compound: 9c
|
Growth inhibition of human MDA-MB-435 cells measured after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-435 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| MDA-MB-468 | GI50 |
0.749 μM
Compound: 9c
|
Growth inhibition of human MDA-MB-468 cells measured after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-468 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| MOLT-4 | GI50 |
0.616 μM
Compound: 9c
|
Growth inhibition of human MOLT-4 cells measured after 48 hrs by SRB assay
Growth inhibition of human MOLT-4 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI/ADR-RES | GI50 |
1.29 μM
Compound: 9c
|
Growth inhibition of human NCI/ADR-RES cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI/ADR-RES cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI-H226 | GI50 |
2.85 μM
Compound: 9c
|
Growth inhibition of human NCI-H226 cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI-H226 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI-H23 | GI50 |
3.41 μM
Compound: 9c
|
Growth inhibition of human NCI-H23 cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI-H23 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI-H322M | GI50 |
1.33 μM
Compound: 9c
|
Growth inhibition of human NCI-H322M cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI-H322M cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI-H460 | GI50 |
1.34 μM
Compound: 9c
|
Growth inhibition of human NCI-H460 cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| NCI-H522 | GI50 |
1.01 μM
Compound: 9c
|
Growth inhibition of human NCI-H522 cells measured after 48 hrs by SRB assay
Growth inhibition of human NCI-H522 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| OVCAR-3 | GI50 |
3.41 μM
Compound: 9c
|
Growth inhibition of human OVCAR-3 cells measured after 48 hrs by SRB assay
Growth inhibition of human OVCAR-3 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| OVCAR-4 | GI50 |
1.57 μM
Compound: 9c
|
Growth inhibition of human OVCAR-4 cells measured after 48 hrs by SRB assay
Growth inhibition of human OVCAR-4 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| OVCAR-5 | GI50 |
2.78 μM
Compound: 9c
|
Growth inhibition of human OVCAR-5 cells measured after 48 hrs by SRB assay
Growth inhibition of human OVCAR-5 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| OVCAR-8 | GI50 |
1.97 μM
Compound: 9c
|
Growth inhibition of human OVCAR-8 cells measured after 48 hrs by SRB assay
Growth inhibition of human OVCAR-8 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| PC-3 | GI50 |
0.805 μM
Compound: 9c
|
Growth inhibition of human PC-3 cells measured after 48 hrs by SRB assay
Growth inhibition of human PC-3 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| RPMI-8226 | GI50 |
1.2 μM
Compound: 9c
|
Growth inhibition of human RPMI-8226 cells measured after 48 hrs by SRB assay
Growth inhibition of human RPMI-8226 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| RXF 393 | GI50 |
0.918 μM
Compound: 9c
|
Growth inhibition of human RXF 393 cells measured after 48 hrs by SRB assay
Growth inhibition of human RXF 393 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SF-268 | GI50 |
1.76 μM
Compound: 9c
|
Growth inhibition of human SF-268 cells measured after 48 hrs by SRB assay
Growth inhibition of human SF-268 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SF-295 | GI50 |
0.803 μM
Compound: 9c
|
Growth inhibition of human SF-295 cells measured after 48 hrs by SRB assay
Growth inhibition of human SF-295 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SF-539 | GI50 |
3.28 μM
Compound: 9c
|
Growth inhibition of human SF-539 cells measured after 48 hrs by SRB assay
Growth inhibition of human SF-539 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SK-MEL-2 | GI50 |
5.3 μM
Compound: 9c
|
Growth inhibition of human SK-MEL-2 cells measured after 48 hrs by SRB assay
Growth inhibition of human SK-MEL-2 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SK-MEL-28 | GI50 |
0.846 μM
Compound: 9c
|
Growth inhibition of human SK-MEL-28 cells measured after 48 hrs by SRB assay
Growth inhibition of human SK-MEL-28 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SK-MEL-5 | GI50 |
1.55 μM
Compound: 9c
|
Growth inhibition of human SK-MEL-5 cells measured after 48 hrs by SRB assay
Growth inhibition of human SK-MEL-5 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SK-OV-3 | GI50 |
4.6 μM
Compound: 9c
|
Growth inhibition of human SK-OV-3 cells measured after 48 hrs by SRB assay
Growth inhibition of human SK-OV-3 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SN12C | GI50 |
1.39 μM
Compound: 9c
|
Growth inhibition of human SN12C cells measured after 48 hrs by SRB assay
Growth inhibition of human SN12C cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SNB-19 | GI50 |
2.1 μM
Compound: 9c
|
Growth inhibition of human SNB-19 cells measured after 48 hrs by SRB assay
Growth inhibition of human SNB-19 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SNB-75 | GI50 |
1.05 μM
Compound: 9c
|
Growth inhibition of human SNB-75 cells measured after 48 hrs by SRB assay
Growth inhibition of human SNB-75 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SR | GI50 |
0.883 μM
Compound: 9c
|
Growth inhibition of human SR cells measured after 48 hrs by SRB assay
Growth inhibition of human SR cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| SW-620 | GI50 |
3.67 μM
Compound: 9c
|
Growth inhibition of human SW-620 cells measured after 48 hrs by SRB assay
Growth inhibition of human SW-620 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| T47D | GI50 |
2.05 μM
Compound: 9c
|
Growth inhibition of human T47D cells measured after 48 hrs by SRB assay
Growth inhibition of human T47D cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| TK-10 | GI50 |
3.47 μM
Compound: 9c
|
Growth inhibition of human TK-10 cells measured after 48 hrs by SRB assay
Growth inhibition of human TK-10 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| U-251 | GI50 |
1.36 μM
Compound: 9c
|
Growth inhibition of human U-251 cells measured after 48 hrs by SRB assay
Growth inhibition of human U-251 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| UACC-257 | GI50 |
1.02 μM
Compound: 9c
|
Growth inhibition of human UACC-257 cells measured after 48 hrs by SRB assay
Growth inhibition of human UACC-257 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| UACC-62 | GI50 |
1.5 μM
Compound: 9c
|
Growth inhibition of human UACC-62 cells measured after 48 hrs by SRB assay
Growth inhibition of human UACC-62 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
| UO-31 | GI50 |
0.746 μM
Compound: 9c
|
Growth inhibition of human UO-31 cells measured after 48 hrs by SRB assay
Growth inhibition of human UO-31 cells measured after 48 hrs by SRB assay
|
[PMID: 32942186] |
Chemical Information
-
CAS No. 2499499-62-4
-
분자량 549.59
-
화학식 C30H30F3N5O2
-
SMILES
CCN1CCN(CC1)C2=CC(C(F)(F)F)=CC(C(NC3=CC=CC(NC4=NC5=CC=CC(OC)=C5C=C4)=C3)=O)=C2
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)