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1446090-77-2 (BGB-283)

1

Identification

BGB-283 BGB-283
Name BGB-283
Formula C25H17F3N4O3
MW 478.42
CAS No. 1446090-77-2
EINECS
Smiles FC(F)(F)C(C=C1)=CC2=C1N=C(N2)[[email protected]@H]3[[email protected]]([[email protected]@H]43)OC(C4=C5)=CC=C5OC6=CC=NC(N7)=C6CCC7=O
Synonyms BGB 283;BGB283; 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one
InChI InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1
2

Introduction

Background Information

BGB-283 is a novel and potent <b>Raf</b> Kinase and <b>EGFR</b> inhibitor with <b>IC<sub>50</sub></b> values of 23 and 29 nM for recombinant BRaf<sup>V600E</sup> and EGFR, respectively. IC50 & Target: IC50: 23 nM (recombinant BRafV600E ), 29 nM (EGFR)<sup>[1]</sup> <i><b>In Vitro:</b></i> BGB-283 potently inhibits BRaf<sup>V600E</sup>-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRaf<sup>V600E</sup> and EGFR mutation/amplification. In BRaf<sup>V600E</sup> colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation<sup>[1]</sup>. <i><b>In Vivo:</b></i> BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRaf<sup>V600E</sup> mutation<sup>[1]</sup>. ......by MedChemexpress Co., Ltd.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000073801

Storage condition

Solubility

DMSO by CHEMSCENE, LLC
DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway
Target Raf EGFR
Research Area Cancer
Indications Solid Tumors
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
BGB-283 BeiGene Solid Tumors 2013/11/1 Phase 1
7

Safety Data of BGB-283

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD130(Get quote);10mg/USD180(Get quote);50mg/USD540(Get quote);100mg/USD840(Get quote) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
10

Related Products

Other Forms of 1446090-77-2

Name CAS No Formula MW

Recommended Compounds in Raf EGFR

Name CAS No Formula MW
HG6-64-1 1315329-43-1 C32H34F3N5O2 577.64
B-Raf inhibitor 1 (dihydrochloride) 1191385-19-9 C26H21Cl3N8 551.86
TAK-632 1228591-30-7 C27H18F4N4O3S 554.52
Dabrafenib (Mesylate) 1195768-06-9 C24H24F3N5O5S3 615.67
LGX818 1269440-17-6 C22H27ClFN7O4S 540.01
B-Raf IN 1 950736-05-7 C29H24F3N5O 515.53
B-Raf inhibitor 1315330-11-0 C29H31F3N6O2 552.59
MLN 2480 1096708-71-2 C17H12Cl2F3N7O2S 506.29
CEP-32496 1188910-76-0 C24H22F3N5O5 517.46
CEP-32496 (hydrochloride) 1227678-26-3 C24H23ClF3N5O5 553.92
Dabrafenib 1195765-45-7 C23H20F3N5O2S2 519.56
B-Raf inhibitor 1 1093100-40-3 C26H19ClN8 478.94
ZM 336372 208260-29-1 C23H23N3O3 389.45
Sorafenib 284461-73-0 C21H16ClF3N4O3 464.83
RAF265 927880-90-8 C24H16F6N6O 518.41
Doramapimod 285983-48-4 C31H37N5O3 527.66
Vemurafenib 918504-65-1 C23H18ClF2N3O3S 489.92
Sorafenib (Tosylate) 475207-59-1 C28H24ClF3N4O6S 637.03
GDC-0879 905281-76-7 C19H18N4O2 334.37
PLX-4720 918505-84-7 C17H14ClF2N3O3S 413.83

Recommended Compounds in Same Indication

Name CAS No Formula MW
MSX-122 897657-95-3 C16H16N6 292.34
NKP-1339 197723-00-5 C14H12Cl4N4NaRu 502.14
NLG-919 1402836-58-1
Gemcitabine elaidate 210829-30-4 C27H43F2N3O5 527.64
Oprozomib 935888-69-0 C25H32N4O7S 532.61
VITAMIN K1 12001-79-5 C31H46O2 450.7
GLPG0187 1320346-97-1 C29H37N7O5S 595.71
Lurbinectedin 497871-47-3 C41H44N4O10S 784.87
D-3263 947257-66-1 C21H31N3O3 373.49
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Route of Synthesis

12

References

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More Information

BGB-283

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