Cat. No.: HY-146443

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.

For research use only. We do not sell to patients.

CAS No.: 2499499-62-4
Formula: C₃₀H₃₀F₃N₅O₂
Molecular Weight:549.59

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

Data Sheet (265 KB)

BRAF V600E/CRAF-IN-2 Chemical Structure

CAS No.: 2499499-62-4

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Biological Activity
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Bioz

Biological Activity

Description

All Raf Isoforms :

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]

Chemical Information

CAS No. 2499499-62-4
Molecular Weight 549.59
Formula 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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (265 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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BRAF V600E/CRAF-IN-2

All Raf Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BRAF V600E/CRAF-IN-2 Related Classifications

HY-146443 Related Classifications