Dabrafenib (GSK2118436)

Name: Dabrafenib (GSK2118436)
Brand: Selleck Chemicals
SKU: S2807
Rating: 5 (174 reviews)

For research use only.

Catalog No.S2807

174 publications

Dabrafenib (GSK2118436) Chemical Structure

CAS No. 1195765-45-7

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Selleck's Dabrafenib (GSK2118436) has been cited by 174 publications

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Nature, 2019, 575(7781):203-209

PubMed: 31666698 ( click the link to review the publication )

Nat Med, 2018, 24(2):203-212

PubMed: 29334371 ( click the link to review the publication )

Cell, 2018, 173(6):1413-1425

PubMed: 29754815 ( click the link to review the publication )

Cancer Discov, 2018, 8(4):417-427

PubMed: 29431697 ( click the link to review the publication )

Nature, 2017, 550(7674):133-136

PubMed: 28953887 ( click the link to review the publication )

Nature, 2017, 551(7679):247-250

PubMed: 29088702 ( click the link to review the publication )

Science, 2016, 352(6282):189-96

PubMed: 27124452 ( click the link to review the publication )

Nat Med, 2016, 22(9):1056-61

PubMed: 27500726 ( click the link to review the publication )

Cancer Cell, 2016, 12;30(3):485-498

PubMed: 27523909 ( click the link to review the publication )

Cancer Discov, 2015, 5(4):358-67

PubMed: 25673644 ( click the link to review the publication )

Cancer Discov, 2014, 4(1):69-79

PubMed: 24265152 ( click the link to review the publication )

Oncogene, 2021, 10.1038/s41388-020-01628-x

PubMed: 33500549 ( click the link to review the publication )

Cell Death Dis, 2021, 12(1):85

PubMed: 33446653 ( click the link to review the publication )

Sci Adv, 2020, 22;6(21):eaaz8521

PubMed: 32494745 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 202004707

PubMed: 32561648 ( click the link to review the publication )

EMBO Rep, 2020, e50163

PubMed: 33369872 ( click the link to review the publication )

Eur J Cancer, 2020, 144:17-30

PubMed: 33316635 ( click the link to review the publication )

Oncogene, 2020, 39(20):4132-4154

PubMed: 32238882 ( click the link to review the publication )

Cancers (Basel), 2020, 12(11)E3205

PubMed: 33143299 ( click the link to review the publication )

Cancers (Basel), 2020, 22;12(2) pii: E512

PubMed: 32098410 ( click the link to review the publication )

Cancers (Basel), 2020, 12(10)E2981

PubMed: 33066704 ( click the link to review the publication )

PLoS Pathog, 2020, 16;16(3):e1008341

PubMed: 32176725 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2020, 10.1111/pcmr.12932

PubMed: 33000894 ( click the link to review the publication )
Cell Death Dis, 2020, 11(11):973

PubMed: 33184267 ( click the link to review the publication )

Cell Commun Signal, 2020, 18(1):156

PubMed: 32967672 ( click the link to review the publication )

ACS Infect Dis, 2020, acsinfecdis.0c00486

PubMed: 33183004 ( click the link to review the publication )

Sci Rep, 2020, 8;10(1):7826

PubMed: 32385388 ( click the link to review the publication )

Sci Rep, 2020, 27;10(1):5557

PubMed: 32221312 ( click the link to review the publication )

J Biol Chem, 2020, 295(8):2407-2420

PubMed: 31929109 ( click the link to review the publication )

Acta Pharmacol Sin, 2020, 13

PubMed: 32404982 ( click the link to review the publication )

Front Chem, 2020, 23;8:184

PubMed: 32266211 ( click the link to review the publication )

Pathol Oncol Res, 2020, 10.1007/s12253-020-00834-y

PubMed: 32591993 ( click the link to review the publication )

Anticancer Res, 2020, 40(4):1867-1874

PubMed: 32234874 ( click the link to review the publication )

Br J Cancer, 2020, 122(6):789-800

PubMed: 31932756 ( click the link to review the publication )

Biology (Basel), 2020, 9(8):E218

PubMed: 32785105 ( click the link to review the publication )

ESMO Open, 2020, 5(4):e000707

PubMed: 32817058 ( click the link to review the publication )

Neoplasia, 2020, 22(9):376-389

PubMed: 32629178 ( click the link to review the publication )

Vet Pathol, 2020, 300985820967449

PubMed: 33205710 ( click the link to review the publication )

Nat Commun, 2020, 11(1):3946

PubMed: 32770055 ( click the link to review the publication )

Oncotarget, 2020, 11(44):3984-3997

PubMed: 33216827 ( click the link to review the publication )

Cancer Cell, 2020, 37(3):387-402

PubMed: 32142667 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 117(49):31105-31113

PubMed: 33229534 ( click the link to review the publication )

Oncotarget, 2020, 11(44):3984-3997

PubMed: 33216827 ( click the link to review the publication )

Acta Neuropathol Commun, 2020, 8(1):139

PubMed: 32811569 ( click the link to review the publication )

Mol Cell, 2019, 76(6):872-884

PubMed: 31606273 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2197

PubMed: 31097693 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5143

PubMed: 31723142 ( click the link to review the publication )
Clin Cancer Res, 2019, 25(21):6429-6442

PubMed: 31439581 ( click the link to review the publication )

Cancer Res, 2019,

PubMed: 31362929 ( click the link to review the publication )

Cell Rep, 2019, 26(1):65-78

PubMed: 30605687 ( click the link to review the publication )

Cell Rep, 2019, 29(3):573-588

PubMed: 31618628 ( click the link to review the publication )

Cell Death Differ, 2019, 10.1038/s41418-019-0298-5

PubMed: 30742091 ( click the link to review the publication )

Eur J Cancer, 2019, 109:137-153

PubMed: 30721788 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):272

PubMed: 31227006 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):56

PubMed: 30728057 ( click the link to review the publication )

Cancers (Basel), 2019, 11(9)

PubMed: 31547367 ( click the link to review the publication )

Cancers (Basel), 2019, 11(9)

PubMed: 31533235 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12824

PubMed: 31518489 ( click the link to review the publication )

Cell Death Dis, 2019, 10(4):281

PubMed: 30911007 ( click the link to review the publication )

Acta Neuropathol Commun, 2019, 7(1):128

PubMed: 31391125 ( click the link to review the publication )

Acta Neuropathol Commun, 2019, 7(1):119

PubMed: 31345255 ( click the link to review the publication )

ACS Chem Biol, 2019, 10.1021/acschembio-00191

PubMed: 31243962 ( click the link to review the publication )

Mol Pharm, 2019, 16(9):3904-3915

PubMed: 31318566 ( click the link to review the publication )

J Virol, 2019, 10.1128/JVI.01791-19

PubMed: 31826996 ( click the link to review the publication )

Biochem Pharmacol, 2019, 169:113616

PubMed: 31445021 ( click the link to review the publication )

Sci Rep, 2019, 9(1):1225

PubMed: 30718660 ( click the link to review the publication )

Cancer Cell Int, 2019, 19:223

PubMed: 31467489 ( click the link to review the publication )

Surgery, 2019, 10.1016/j.surg.2019.04.076

PubMed: 31585718 ( click the link to review the publication )

Acta Pharmacol Sin, 2019, 40(2):268-278

PubMed: 29777202 ( click the link to review the publication )

Metabolites, 2019, 9(11)

PubMed: 31744229 ( click the link to review the publication )

Chembiochem, 2019, 10.1002/cbic.201900266

PubMed: 31152574 ( click the link to review the publication )
PLoS One, 2019, 14(6):e0217399

PubMed: 31158244 ( click the link to review the publication )

Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520

PubMed: 31618797 ( click the link to review the publication )

Reprod Domest Anim, 2019, 54(5):741-749

PubMed: 30785650 ( click the link to review the publication )

Target Oncol, 2019, 14(5):619-626

PubMed: 31502118 ( click the link to review the publication )

Sci Adv, 2019, 5(8):eaav8463

PubMed: 31453322 ( click the link to review the publication )

Mol Ther Nucleic Acids, 2019, 14:287-300

PubMed: 30654190 ( click the link to review the publication )

Ann Biomed Eng, 2019, 10.1007/s10439-019-02269-2

PubMed: 31020445 ( click the link to review the publication )

Sci Rep, 2019, 9(1):10865

PubMed: 31350469 ( click the link to review the publication )

Exp Gerontol, 2019, 126:110691

PubMed: 31421186 ( click the link to review the publication )

Int J Mol Sci, 2019, 20(23)

PubMed: 31783660 ( click the link to review the publication )

Transl Oncol, 2019, 13(2):275-286

PubMed: 31874374 ( click the link to review the publication )

Nat Biomed Eng, 2018, 2(8):578-588

PubMed: 31015631 ( click the link to review the publication )

Nat Biomed Eng, 2018, 2(4):239-253

PubMed: 30936439 ( click the link to review the publication )

Mol Cell, 2018, 69(6):923-937

PubMed: 29547721 ( click the link to review the publication )

Mol Cell, 2018, 70(5):920-935

PubMed: 29883609 ( click the link to review the publication )

Nat Protoc, 2018, 13(12):2827-2843

PubMed: 30382243 ( click the link to review the publication )

Nat Commun, 2018, 9(1):3440

PubMed: 30143629 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2500

PubMed: 29950559 ( click the link to review the publication )

Nat Commun, 2018, 9(1):1466

PubMed: 29654229 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(5):1090-1102

PubMed: 29196297 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(14):3377-3385

PubMed: 29650750 ( click the link to review the publication )

Cancer research, 2018, 78(2):542-557

PubMed: 29180473 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(23):6066-6077

PubMed: 30061362 ( click the link to review the publication )

Breast Cancer Res, 2018, 20(1):9

PubMed: 29382358 ( click the link to review the publication )
Cell Chem Biol, 2018, 25(2):175-184

PubMed: 29249695 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):84-95

PubMed: 29133617 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(4):806-813

PubMed: 29167314 ( click the link to review the publication )

Mol Oncol, 2018, 12(1):74-88

PubMed: 29112787 ( click the link to review the publication )

Neoplasia, 2018, 20(5):467-477

PubMed: 29605720 ( click the link to review the publication )

Hum Mol Genet, 2018, 27(22):3974-3985

PubMed: 30137437 ( click the link to review the publication )

Oncogenesis, 2018, 7(9):67

PubMed: 30190455 ( click the link to review the publication )

Sci Rep, 2018, 8(1):9991

PubMed: 29968772 ( click the link to review the publication )

Front Pharmacol, 2018, 9:856

PubMed: 30154717 ( click the link to review the publication )

ACS Med Chem Lett, 2018, 9(12):1199-1204

PubMed: 30613326 ( click the link to review the publication )

Acta Biochim Biophys Sin (Shanghai), 2018, 50(4):355-361

PubMed: 29534162 ( click the link to review the publication )

Anticancer Res, 2018, 38(11):6195-6200

PubMed: 30396937 ( click the link to review the publication )

Oncotarget, 2018, 9(92):36503-36514

PubMed: 30559933 ( click the link to review the publication )

Cell Death Dis, 2018, 9(3):325

PubMed: 29487283 ( click the link to review the publication )

Oncotarget, 2018, 9(17):13324-13336

PubMed: 29568360 ( click the link to review the publication )

Small GTPases, 2018, 10.1080/21541248.2018.1446697

PubMed: 29634387 ( click the link to review the publication )

Sci Rep, 2018, 8(1):10724

PubMed: 30013176 ( click the link to review the publication )

NPJ Syst Biol Appl, 2018, 4:39

PubMed: 30416750 ( click the link to review the publication )

Oncoimmunology, 2018, 8(1):e1512456

PubMed: 30546949 ( click the link to review the publication )

Cell Syst, 2018, 7(2):161-179

PubMed: 30007540 ( click the link to review the publication )

Oncotarget, 2018, 9(51):29680-29697

PubMed: 30038713 ( click the link to review the publication )

Oncotarget, 2018, 9(47):28294-28308

PubMed: 29983861 ( click the link to review the publication )

Neural Regen Res, 2018, 13(2):252-256

PubMed: 29557374 ( click the link to review the publication )

Nat Commun, 2017, 8:15623

PubMed: 28585535 ( click the link to review the publication )
Nat Commun, 2017, 8(1):823

PubMed: 29018192 ( click the link to review the publication )

Cancer Res, 2017, 77(17):4684-4696

PubMed: 28652244 ( click the link to review the publication )

Cell Mol Life Sci, 2017, 74(19):3631-3645

PubMed: 28551825 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )

Transl Lung Cancer Res, 2017, 6(5):600-610

PubMed: 29114475 ( click the link to review the publication )

Sci Rep, 2017, 7(1):15523

PubMed: 29138474 ( click the link to review the publication )

Anal Bioanal Chem, 2017, 409(15):3749-3756

PubMed: 28429064 ( click the link to review the publication )

Oncol Rep, 2017, 38(5):2741-2751

PubMed: 29048639 ( click the link to review the publication )

Biochem Biophys Res Commun, 2017, 489(1):14-20

PubMed: 28536078 ( click the link to review the publication )

Oncotarget, 2017, 8(40):68208-68220

PubMed: 28978109 ( click the link to review the publication )

Oncotarget, 2017, 8(64):107977-107990

PubMed: 29296217 ( click the link to review the publication )

Biochim Biophys Acta Gen Subj, 2017, 1861(11 Pt B):2980-2992

PubMed: 28408301 ( click the link to review the publication )

Cell Death Differ, 2017, 24(1):83-97

PubMed: 27834956 ( click the link to review the publication )

Genome Res, 2017, 27(4):613-625

PubMed: 28179366 ( click the link to review the publication )

Oncogene, 2017, 36(27):3842-3851

PubMed: 28263969 ( click the link to review the publication )

Elife, 2017, 6

PubMed: 28350298 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2017, 114(29):E5930-E5939

PubMed: 28684402 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(10)

PubMed: 29064427 ( click the link to review the publication )

Oncotarget, 2017, 8(52):90262-90277

PubMed: 29163826 ( click the link to review the publication )

Oncotarget, 2017, 9(9):8206-8222

PubMed: 29492189 ( click the link to review the publication )

Blood Adv, 2017, 30;1(24):2147-2160

PubMed: 29296862 ( click the link to review the publication )

Nat Commun, 2016, 7:10274

PubMed: 26817517 ( click the link to review the publication )

Autophagy, 2016, 12(10):1776-1790

PubMed: 27464255 ( click the link to review the publication )

Leukemia, 2016, 30(4):937-46

PubMed: 26582644 ( click the link to review the publication )
Mol Cancer Ther, 2016, 10.1158/1535-7163.MCT-15-0375

PubMed: 27196768 ( click the link to review the publication )

J Biol Chem, 2016, 291(34):17804-15

PubMed: 27226552 ( click the link to review the publication )

Cancer Biol Ther, 2016, 17(7):778-84

PubMed: 26810603 ( click the link to review the publication )

PLoS One, 2016, 11(3):e0152104

PubMed: 27015094 ( click the link to review the publication )

Oncotarget, 2016, 8(35):58021-58036

PubMed: 28938534 ( click the link to review the publication )

Oncotarget, 2016, 7(21):30453-60

PubMed: 27028853 ( click the link to review the publication )

Sci Rep, 2016, 6:23713

PubMed: 27025703 ( click the link to review the publication )

Elife, 2016, 5

PubMed: 27557444 ( click the link to review the publication )

Oncotarget, 2016, 7(46):75839-75853

PubMed: 27713119 ( click the link to review the publication )

Oncotarget, 2016, 7(12):15065-92

PubMed: 26918341 ( click the link to review the publication )

Cell Res, 2015, 10.1038/cr.2015.56

PubMed: 25952668 ( click the link to review the publication )

Mol Ther, 2015, 23(5):931-942

PubMed: 25619724 ( click the link to review the publication )

J Invest Dermatol, 2015, 135(8):2021-2030

PubMed: 25748555 ( click the link to review the publication )

Antimicrob Agents Chemother, 2015, 59(2):1088-99

PubMed: 25487801 ( click the link to review the publication )

J Immunother, 2015, 38(1):12-23

PubMed: 25415284 ( click the link to review the publication )

Eur J Pharmacol, 2015, 762:283-92

PubMed: 26048310 ( click the link to review the publication )

PLoS One, 2015, 10(12):e0143847

PubMed: 26630652 ( click the link to review the publication )

PLoS One, 2015, 10(4):e0123410

PubMed: 25844720 ( click the link to review the publication )

Cancer Res, 2015, 75(1):216-29

PubMed: 25381152 ( click the link to review the publication )

Drug Metab Dispos, 2015, 43(12):1934-7

PubMed: 26443648 ( click the link to review the publication )

Oncotarget, 2015, 6(38):40535-56

PubMed: 26497853 ( click the link to review the publication )

Cancer Immunol Res, 2015, 3(6):602-9

PubMed: 25795007 ( click the link to review the publication )

Oncotarget, 2015, 6(31):31792-804

PubMed: 26397139 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(12):2700-11

PubMed: 26351322 ( click the link to review the publication )
J Clin Invest, 2014, 124(3):1406-17

PubMed: 24569374 ( click the link to review the publication )

J Clin Invest, 2014, 124(11):5074-84

PubMed: 25329694 ( click the link to review the publication )

Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1392

PubMed: 25297634 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1278

PubMed: 24901049 ( click the link to review the publication )

Transl Res, 2014, 164(5):411-23

PubMed: 25016932 ( click the link to review the publication )

The University of Texas, 2014, Lizee S

PubMed: ( click the link to review the publication )

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Targets

B-Raf (V600E) ^[3] (Cell-free assay)	B-Raf ^[3] (Cell-free assay)	C-Raf ^[3] (Cell-free assay)
0.7 nM	5.2 nM	6.3 nM

In vitro

Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-Raf^V600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-Raf^V600E. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
	Mnv6T4lv[XOnIFHzd4F6				MWfJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiSHnzJJRi\2enZDDCMXJi\iCYNkCwSUBufXSjboSg[ZhxemW\|c3XkJIlvKGKjY4Xsc5ZqenW\|IHnu[oVkfGWmIHnud4VkfCClZXzsd{Bkdy2neIDy[ZN{cW6pIFPER\|M4KGG\|c3Xzd4VlKGG\|IHTlZ5Jm[XOnIHnuJIJqd3SrbonsZZRm\C2PRVugdJJwfGWrbjDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO\|YYmge4l1cCCLQ{WwJI9nKDBwMECwO{DPxE1?	NYD5bJUzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd\|PD;hQi=>
SK-MEL-28	M2rFWWtqdmG\|ZTDBd5NigQ>?		Ml3SNUBp		M3\IXWlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIGPLMW1GVC1{ODDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG\|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxPCEQvF2=	NXjkOJZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd\|PD;hQi=>
HepG2	NIH2RpdMcW6jc3WgRZN{[Xl?				NGfRS5pKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDFVmsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCwOEDPxE1?	NYSwTGN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd\|PD;hQi=>
COLO205	NVzBTHZWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NGPDeJNKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:yNFUh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O\|M9N2F-
HepG2	MoDSSpVv[3Srb36gRZN{[Xl?		NGXuSVI1PSCvaX6=	M{S5VWROW09?	NUO2UpRXUW6qaXLpeIlwdiCxZjDBcIs2KGmwIGTHSk1j\XSjLYP0bY12dGG2ZXSgbJVu[W5iSHXwS\|Ih[2WubIOgZZN{\XO\|ZXSgZZMh\GWlcnXhd4UhcW5iU33h[FIheGixc4Doc5J6dGG2aX;uJJRz\WG2ZXSg[o9zKDR3IH3pcpMheHKrb4KgeI8hXEeILXLleIEhe3SrbYXsZZRqd25ibXXhd5Vz\WRiYX\0[ZIhPjBibXnud{BjgSCxZInzd4V6KGKub4Sgd4Nidm6ncjDhcoFtgXOrczD3bZRpKEmFNUCgc4YhOy55IN88US=>	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O\|M9N2F-
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CAL-27	MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4TEWFExKM7:TR?=	M4XCb\|czKGh?	NEPVeo5FVVOR	NVvTcWdLUUN3ME2xNEDPxE1?	M3rhclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
CAL-62	NXrDO\|BJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFHXZXMyOCEQvF2=	NFW5Rlc4OiCq	NILLUYFFVVOR	M3v5NGlEPTB;MUCg{txO	NWDSPVNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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CaOV3	M1zDcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3LRS\|ExKM7:TR?=	MYi3NkBp	Mk\NSG1UVw>?	MWfJR\|UxRTFyIN88US=>	NYjlSnR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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CHL-1	M2XERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV:xNEDPxE1?	MYS3NkBp	M3WxWmROW09?	MkXYTWM2OD1zMDFOwG0>	NGTUPVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
Colo320DM	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVWxNEDPxE1?	NETNb5k4OiCq	M1\G[WROW09?	NUnD[\|ZWUUN3ME2xNEDPxE1?	M1XrPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
Colo704	NH\zNpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXXr[I9KOTBizszN	Ml2zO\|IhcA>?	M{LiVWROW09?	M2K5Z2lEPTB;MUCg{txO	M3;5SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
COR-L23	MmPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3vYVlExKM7:TR?=	Ml;CO\|IhcA>?	MmexSG1UVw>?	M2fES2lEPTB;MUCg{txO	NXnLc\|h1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
CRO-AP2	MojLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVniNHhEOTBizszN	Mnr6O\|IhcA>?	MVTEUXNQ	NXP3R41oUUN3ME2xNEDPxE1?	MkPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN\|goRjJ\|OES0NFM5RC:jPh?=
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DU-145	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2rRTFExKM7:TR?=	Mkf6O\|IhcA>?	Mn\USG1UVw>?	M2TjPWlEPTB;MUCg{txO	NUnqd3VMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
EB-3	NV:yc5BsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1r5flExKM7:TR?=	NE\pS2c4OiCq	NU\MOXVJTE2VTx?=	NVnDcYRlUUN3ME2xNEDPxE1?	NH3nTlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
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G401	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3nKSFExKM7:TR?=	NYLLWlRFPzJiaB?=	NX\0VlRbTE2VTx?=	MXrJR\|UxRTFyIN88US=>	M2GyS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
HCC-70	NXXKT2pRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3L5eVExKM7:TR?=	MlnrO\|IhcA>?	NGnDUGxFVVOR	NFKyVpBKSzVyPUGwJO69VQ>?	M1vUOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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Hela	NFu5TXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUexNEDPxE1?	MorsO\|IhcA>?	NHXjTWpFVVOR	MXnJR\|UxRTFyIN88US=>	NUX0O\|Q1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
Hep3B	M4WwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXewOVdGOTBizszN	MnnsO\|IhcA>?	NVPFenZOTE2VTx?=	MVXJR\|UxRTFyIN88US=>	NFPNOpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
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HN5	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWGxNEDPxE1?	MoXNO\|IhcA>?	M334UWROW09?	M2HOZmlEPTB;MUCg{txO	M2TseFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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HPAF-II	NGjlflFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEfySm8yOCEQvF2=	MUO3NkBp	M3:2fmROW09?	NVPrWW9pUUN3ME2xNEDPxE1?	NEHnVo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
Hs746.T	NE\IS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUjQV5dbOTBizszN	NWHNRmRLPzJiaB?=	MkTySG1UVw>?	MnPJTWM2OD1zMDFOwG0>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
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IGROV1	NH7S[\|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVTuWYhCOTBizszN	M2nQR\|czKGh?	NETqPW9FVVOR	MonITWM2OD1zMDFOwG0>	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
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Kato III	NFKyRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX3GT\|FGOTBizszN	NFHVZ3Y4OiCq	NGrvOHpFVVOR	MoHsTWM2OD1zMDFOwG0>	M37xPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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KM-12	NUDob3dCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NH\YdGEyOCEQvF2=	NWXxfYJOPzJiaB?=	MV7EUXNQ	MXfJR\|UxRTFyIN88US=>	NWfWPIxORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
KPL-1	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYmxNEDPxE1?	NHnOdmI4OiCq	NY\BXlRzTE2VTx?=	NIDU[mVKSzVyPUGwJO69VQ>?	M3y1c\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OES0NFM5Lz5{M{i0OFA{QDxxYU6=
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Molt-4	NEiwfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXXpTlBCOTBizszN	MXq3NkBp	Mlv1SG1UVw>?	NWrUTXNlUUN3ME2xNEDPxE1?	NFzZWnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0OFA{QCd-MkO4OFQxOzh:L3G+
NCI-ADR/RES	NEnabmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4W1TlExKM7:TR?=	NHu0bW84OiCq	M4OwNGROW09?	MkX3TWM2OD1zMDFOwG0>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
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NCI-H146	NGftelJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUTMbnd6OTBizszN	MlPRO\|IhcA>?	MYrEUXNQ	NGrhXI1KSzVyPUGwJO69VQ>?	NWi2NmNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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NCI-H187	NUT1NIJlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIizVmUyOCEQvF2=	MnP2O\|IhcA>?	NIDRVXZFVVOR	NVviemptUUN3ME2xNEDPxE1?	NUfNcFNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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NCI-H226	NGDlOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXzHd2Z7OTBizszN	NGj0WIw4OiCq	NX7Tfmd4TE2VTx?=	MWjJR\|UxRTFyIN88US=>	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NECzPEc,OjN6NESwN\|g9N2F-
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SK-MEL-28	NHzHdZFEgXSxdH;4bYNqfHliYYPzZZk>		NFjGfoo1QCCq		NUjtcmZwS3m2b4P0ZZRq[yCjY4Tpeol1gSCrbjDoeY1idiCVSz3NSWwuOjhiY3XscJMhcGG{Yn;ybY5oKEKUQV[gWlYxOEVibYX0ZY51KGG2IEGgZY5lKDNyIIXNJI1m[XO3cnXkJIFnfGW{IES4JIhzeyC{ZYPhfpVzcW5iYYPzZZk>	M2XBSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{e0NVM4Lz5{N{e3OFE{PzxxYU6=
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NB1643	NGG4fo5RemmvYYL5JJNkemWnbjDhd5NigQ>?				MkK2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?=	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	NEnoeopRemmvYYL5JJNkemWnbjDhd5NigQ>?				MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NV7tToU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pMEK / pERK / ERK; PubMed: 31158244 PLoS One Cell lines as shown were treated with dabrafenib, over a dose range, for 1 hour. UT = untransfected. Expression and/or phosphorylation of the indicated proteins were assessed by immunoblot. p-S6 / p-AKT308 / p-AKT473; PubMed: 24735930 Mol Cancer Western blot analysis of phosphorylated proteins in MAPK and the PI3K-AKT pathway after 24 hours exposure to increasing concentrations of dabrafenib. β-catenin; PubMed: 29167314 Mol Cancer Ther HT-29 cells were treated with BRAF inhibitors Dabrafenib (2 μM), GDC-0879 (4 μM) or Vemurafenib (2 μM) for indicated times. The whole cell lysates were used for western blot with indicated antibodies.	31158244 24735930 29167314
Growth inhibition assay	IC50; PubMed: 24735930 Mol Cancer A panel of 23 BRAF(V600) mutant human melanoma cell lines was treated with serial dilutions (1-10,000 nM) of dabrafenib (A) for 72-120 hours to assess cell viability. The bars represent the average IC50 value of two or more independent experiments in duplicates and the error bars represent the SEM.	24735930

In vivo

Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. ^[1]

Protocol

References

Solubility (25°C)

In vitro	DMSO	30 mg/mL (57.74 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+45% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing.	5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Dabrafenib (GSK2118436) SDF

Molecular Weight	519.56
Formula	C₂₃H₂₀F₃N₅O₂S₂
CAS No.	1195765-45-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04547946	Not yet recruiting	Drug: dabrafenib + trametinib	Malignant Melanoma	Novartis Pharmaceuticals\|Novartis	January 29 2021	--
NCT04666272	Not yet recruiting	Drug: dabrafenib\|Drug: trametinib	Melanoma	Novartis Pharmaceuticals\|Novartis	December 22 2020	--
NCT04452877	Recruiting	Drug: Dabrafenib\|Drug: Trametinib	Carcinoma Non-Small-Cell Lung	Novartis Pharmaceuticals\|Novartis	August 19 2020	Phase 2
NCT04059224	Recruiting	Drug: Trametinib\|Drug: Dabrafenib	Stage IV Melanoma\|Stage III Melanoma	Universitair Ziekenhuis Brussel	January 28 2019	Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

Pan Raf Inhibitor

AZ 628 : Pan-Raf inhibitor, BRAF, IC50=105 nM; BRAFV600E, IC50=34 nM; c-Raf-1, IC50=29 nM.
FDA-approved Raf Inhibitor

Sorafenib Tosylate : Approved by FDA for advanced renal cancer。
Newest Raf Inhibitor

TAK-632 ^New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

Related Raf Products

LY3009120 ^New

LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Ravoxertinib (GDC-0994) ^New

Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Ulixertinib (BVD-523) ^New

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Vemurafenib (PLX4032)

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.

Features:A novel and potent inhibitor of the B-RAF^V600E oncoprotein.
Sorafenib

Sorafenib (BAY 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Sorafenib Tosylate

Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
PLX-4720

PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
TAK-632

TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.
GDC-0879

GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
GW5074

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.

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Dabrafenib (GSK2118436)