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Datasheet of Sorafenib

Description:
Sorafenib tosylate (BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf,
and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.
Sorafenib is a drug approved for the treatment of primary kidney cancer (advanced renal cell carcinoma) and advanced primary
liver cancer (hepatocellular carcinoma).
in vitro: Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM,
respectively. Sorafenib tosylate also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFR, Flt3, and c-Kit with IC50 of
15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib tosylate weakly inhibits FGFR-1 with IC50 of 580 nM.
Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKC, PKC,
and pim-1. Sorafenib tosylate markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3
phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib tosylate potently blocks MEK 1/2 and ERK 1/2
phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway.
Sorafenib tosylate inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 M and 2.6 M, respectively.
Persistent activation of AMPK by sorafenib finally led to the impairment of glucose metabolism both in MCF-7 and SKBR3 cells
as well as in the highly glycolytic MDA-MB-231 cells, resulting in cell death.
in vivo: The number of S-phase nuclei and mitotic indices decreased 48 h after PH and increased 7 d after PH in animals on
sorafenibtreatment. Relative liver weights were restored 5 d after PH in control rats, at 7 d in animals receiving sorafenib prior to
surgery, at 10 d in rats wheresorafenib was stopped 3 d after surgery, and after 14 d in rats on continuous treatment [3]. From day
7 after LT, sorafenib was administrated at 30 mg/kg/day for 3 weeks. Our results showed that the serum levels of vascular
endothelial growth factor and hepatocyte growth factor significantly increased after LT, and the T helper 1 (T(h)1)/T helper 2
(T(h)2) immune balance was shifted toward a T(h)2 response after immunosuppressant administration.

Chemical Information
Catalog

DC2098

Purity of current batch:

>98%

Molecular Weight (MW)

637.03

Molecular Formula

C21H16ClF3N4O3.C7H8O3S

CAS No.

475207-59-1

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.