BRAF V600E/CRAF-IN-2

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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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BRAF V600E/CRAF-IN-2 Chemical Structure

CAS No. : 2499499-62-4

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BRaf c-Raf Raf

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

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]

Molecular Weight

549.59

Formula

C₃₀H₃₀F₃N₅O₂

CAS No.

2499499-62-4

SMILES

CCN1CCN(CC1)C2=CC(C(F)(F)F)=CC(C(NC3=CC=CC(NC4=NC5=CC=CC(OC)=C5C=C4)=C3)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. El-Damasy AK,et al. 2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAFV600E/C-RAF kinase inhibitory effects: Design, synthesis, in vitro cell-based and oncogenic kinase assessments. Eur J Med Chem. 2020 Dec 15;208:112756. [Content Brief]