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索拉非尼 /Sorafenib {[allProObj[0].p_purity_real_show]}

货号:A316727 同义名: Bay 43-9006

Sorafenib is a multi-kinase inhibitor that inhibits Raf-1 and B-RAF (IC50s = 6 and 22 µM, respectively), as well as the receptor tyrosine kinases VEGFR2, VEGFR3, PDGFRβ, FLT3, and c-Kit (IC50s = 90, 15, 20, 57, and 58 nM, respectively).

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Sorafenib 化学结构 CAS号:284461-73-0
Sorafenib 化学结构
CAS号:284461-73-0
Sorafenib 3D分子结构
CAS号:284461-73-0
Sorafenib 化学结构 CAS号:284461-73-0
Sorafenib 3D分子结构 CAS号:284461-73-0
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Sorafenib 纯度/质量文件 产品仅供科研

货号:A316727 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 c-Kit 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

98%
Ki8751 ++

c-Kit, IC50: 40 nM

98+%
Tivozanib ++

c-Kit, IC50: 78 nM

99%+
Pazopanib +

c-Kit, IC50: 140 nM

99%
Sitravatinib +++

Kit, IC50: 6 nM

99%+
Pexidartinib +++

Kit, IC50: 10 nM

99%+
Lactate ++++

c-Kit, IC50: 2 nM

FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

98%
Axitinib ++++

Kit, IC50: 1.7 nM

98%
Dovitinib ++++

c-Kit, IC50: 2 nM

FLT3 99%+
Sunitinib FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

99%+
Telatinib ++++

c-Kit, IC50: 1 nM

99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

Src 98%
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 PDGFR PDGFRα PDGFRβ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

98%
Pazopanib ++

PDGFR, IC50: 84 nM

99%
Imatinib +

PDGFR, IC50: 100 nM

c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

c-Kit 99%
Sennoside B 99%+
PP121 ++++

PDGFR, IC50: 2 nM

VEGFR,mTOR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

++++

PDGFRβ, Kd: 3.2 nM

99%+
Masitinib +

PDGFRα, IC50: 540 nM

+

PDGFRβ, IC50: 800 nM

99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

c-Kit 98+%
Tivozanib ++

PDGFRα, IC50: 40 nM

++

PDGFRβ, IC50: 49 nM

99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

++++

PDGFRβ, IC50: 1.6 nM

98%
CP-673451 +++

PDGFRα, IC50: 10 nM

++++

PDGFRβ, IC50: 1 nM

99%+
Telatinib +++

PDGFRα, IC50: 15 nM

c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

++

PDGFRβ, IC50: 65 nM

99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

98%+
Lactate +++

PDGFRβ, IC50: 27 nM

FLT3,c-Kit 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

FLT3,c-Kit 99%+
Sorafenib ++

mPDGFRβ, IC50: 57 nM

PDGFRβ, IC50: 57 nM

99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 FLT3 其他靶点 纯度
R406 Syk 98%
Go6976 99%+
Quizartinib +++

FLT3 (WT), IC50: 4.2 nM

FLT3 (ITD), IC50: 1.1 nM

98%
Gilteritinib ++++

FLT3, IC50: 0.29 nM

99%+
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

99%+
Pacritinib ++

FLT3 (D835Y), IC50: 6 nM

FLT3, IC50: 22 nM

97%
Dovitinib ++++

FLT3, IC50: 1 nM

c-Kit 99%+
Denfivontinib ++++

FLT3 (D835Y), IC50: 0.4 nM

FLT3, IC50: 0.4 nM

RET 99%+
TAK-659 HCl ++

FLT3, IC50: 4.6 nM

Syk 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 A-raf B-Raf C-Raf/Raf-1 Raf 其他靶点 纯度
Encorafenib 99%+
GDC-0879 ++++

B-Raf, IC50: 0.13 nM

99%+
SB-590885 ++++

B-Raf, Ki: 0.16 nM

99%+
RAF265 99%+
Dabrafenib ++++

B-Raf, IC50: 5.2 nM

B-Raf (V600E), IC50: 0.7 nM

+++

C-Raf, IC50: 6.3 nM

98%
Lifirafenib ++++

WT A-RAF, IC50: 1 nM

++

BRAF(V600E), IC50: 23 nM

BRAF WT, IC50: 32 nM

+++

C-RAF (Y340/341D), IC50: 7 nM

EGFR 98%
ZM 336372 +

C-Raf, IC50: 70 nM

99%+
NVP-BHG 712 +

C-Raf, IC50: 0.395 μM

99%+
CCT196969 +

BRAF, IC50: 0.1 μM

++

CRAF, IC50: 0.01 μM

Src 98%
Vemurafenib ++

B-Raf, IC50: 100 nM

B-Raf (V600E), IC50: 31 nM

+

C-Raf, IC50: 48 nM

98+%
PLX4720 ++

B-Raf, IC50: 160 nM

B-Raf (V600E), IC50: 13 nM

+++

C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM

BRK 99+%
GW 5074 +++

C-Raf, IC50: 9 nM

99%+
Avutometinib +++

BRAF, IC50: 19 nM

BRAF V600E, IC50: 8.2 nM

+

CRAF, IC50: 56 nM

98%
LY3009120 ++++

BRAF(V600E), IC50: 5.8 nM

BRAF WT, IC50: 15 nM

++++

C-Raf, IC50: 4.3 nM

99%+
Agerafenib ++

B-Raf, Kd: 36 nM

B-Raf (V600E), Kd: 14 nM

+

C-Raf, Kd: 39 nM

RET 99%+
TAK-632 +++

B-Raf, IC50: 8.3 nM

++++

C-Raf, IC50: 1.4 nM

99%+
AZ 628 +

B-Raf, IC50: 105 nM

B-Raf (V600E), IC50: 34 nM

++

C-Raf-1, IC50: 29 nM

99%
PLX7904 98+%
Sorafenib ++

B-Raf (V599E), IC50: 38 nM

B-Raf, IC50: 22 nM

++++

Raf-1, IC50: 6 nM

++++

Raf-1, IC50: 6 nM

99%
Tovorafenib 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 VEGFR1 VEGFR2 VEGFR3 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

++++

VEGFR2, IC50: 3 nM

VEGFR2/Flk1, IC50: 3 nM

+++

VEGFR3, IC50: 6 nM

PDGFR,RET 98%
Tivozanib ++

VEGFR1, IC50: 30 nM

+++

VEGFR2, IC50: 6.5 nM

++

VEGFR3, IC50: 15 nM

99%+
Brivanib +

VEGFR1, IC50: 380 nM

++

VEGFR2, IC50: 25 nM

Flk1, IC50: 25 nM

99%+
Regorafenib +++

VEGFR1, IC50: 13 nM

+++

VEGFR2, IC50: 4.2 nM

+

VEGFR3, IC50: 46 nM

RET 98%
Pazopanib +++

VEGFR1, IC50: 10 nM

++

VEGFR2, IC50: 30 nM

+

VEGFR3, IC50: 47 nM

FGFR,PDGFR,c-Kit 99%
Sitravatinib +++

VEGFR1 (FLT1), IC50: 6 nM

+++

VEGFR2 (KDR), IC50: 5 nM

++++

VEGFR3 (FLT4), IC50: 2 nM

99%+
Foretinib +++

VEGFR1/FLT1, IC50: 6.8 nM

++++

KDR, IC50: 0.86 nM

++++

VEGFR3/FLT4, IC50: 2.8 nM

Tie-2 99%+
MGCD-265 analog ++++

VEGFR1, IC50: 3 nM

++++

VEGFR2, IC50: 3 nM

++++

VEGFR3, IC50: 4 nM

Tie-2 99%+
Lactate +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

FLT3,c-Kit 85%
AEE788 +

FLT1, IC50: 59 nM

+

KDR, IC50: 77 nM

EGFR 98+%
Linifanib ++++

VEGFR1/FLT1, IC50: 3 nM

++++

VEGFR2/KDR, IC50: 4 nM

+

VEGFR3/FLT4, IC50: 190 nM

FLT3 99%+
Vatalanib 2HCl +

VEGFR1/FLT1, IC50: 77 nM

++

VEGFR2/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

+

VEGFR3/FLT4, IC50: 660 nM

c-Kit,c-Fms 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 nM

98%
Dovitinib +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

FLT3,c-Kit 99%+
ZM 306416 +

VEGFR1, IC50: 0.33 μM

Src 99%+
KRN-633 +

VEGFR1, IC50: 170 nM

+

VEGFR2, IC50: 160 nM

+

VEGFR3, IC50: 125 nM

c-Kit,BTK 98%
OSI-930 +++

FLT1, IC50: 8 nM

+++

KDR, IC50: 9 nM

99%+
Lenvatinib ++

VEGFR1/FLT1, IC50: 22 nM

++++

VEGFR2/KDR, IC50: 4.0 nM

+++

VEGFR3/FLT4, IC50: 5.2 nM

98%
NVP-BAW2881 +

hVEGFR1, IC50: 820 nM

+++

mVEGF2, IC50: 165 nM

hVEGFR2, IC50: 9 nM

+

hVEGFR3, IC50: 420 nM

98%
Cediranib +++

VEGFR1/FLT1, IC50: 5 nM

++++

VEGFR2/KDR, IC50: 0.5 nM

c-Kit 99%+
Nintedanib ++

VEGFR1, IC50: 34 nM

+++

VEGFR2, IC50: 13 nM

+++

VEGFR3, IC50: 13 nM

FLT3 99+%
BMS-794833 ++

VEGFR2, IC50: 15 nM

99%+
SKLB1002 ++

VEGFR2, IC50: 32 nM

98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 98+%
SU 5402 ++

VEGFR2, IC50: 20 nM

98%
Rivoceranib Mesylate ++++

VEGFR2, IC50: 1 nM

RET 98+%
Ponatinib ++++

VEGFR2, IC50: 1.5 nM

98%
LY2874455 +++

VEGFR2, IC50: 7 nM

99%+
ZM323881 HCl ++++

VEGFR2, IC50: <2 nM

98%
AZD2932 +++

VEGFR-2, IC50: 8 nM

c-Kit 98%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

98%
Sorafenib ++

VEGFR2, IC50: 90 nM

VEGFR2/Flk1, IC50: 90 nM

99%
CYC-116 ++

VEGFR2, Ki: 44 nM

FLT3 99%+
Golvatinib ++

VEGFR2, IC50: 16 nM

99%+
Sunitinib +

VEGFR2 , IC50: 80 nM

FLT3 98%
RAF265 ++

VEGFR2, EC50: 30 nM

99%+
PD173074 99%+
BFH772 ++++

VEGFR2, IC50: 3 nM

98%
Semaxinib +

VEGFR2/Flk1, IC50: 1.23 μM

98%
Vandetanib ++

VEGFR2, IC50: 40 nM

+

VEGFR3, IC50: 110 nM

EGFR 98%
SAR131675 ++

VEGFR3, IC50: 23 nM

99%+
ENMD-2076 +

VEGFR2/KDR, IC50: 58.2 nM

++

VEGFR3/FLT4, IC50: 15.9 nM

FLT3,RET 98%
Telatinib +++

VEGFR2, IC50: 6 nM

++++

VEGFR3, IC50: 4 nM

c-Kit 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Sorafenib 生物活性

靶点
  • VEGFR2

    VEGFR2, IC50:90 nM

    VEGFR2/Flk1, IC50:90 nM

  • PDGFRβ

    mPDGFRβ, IC50:57 nM

    PDGFRβ, IC50:57 nM

  • FGFR1

    FGFR1, IC50:580 nM

  • B-Raf

    B-Raf (V599E), IC50:38 nM

    B-Raf, IC50:22 nM

描述 The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Sorafenib is a multitargeted inhibitor with IC50 values of 6nM, 22nM and 38nM for Raf-1, wt-BRAF and BRAF-V599E mutant, respectively, as well as less potent to mVEGFR2, mVEGFR3, mPDGFRβ, FLT3, c-Kit, VEGFR2 and FGFR1 with IC50 values of 15nM, 20nM, 57nM, 58nM, 68nM, 90nM and 580nM (measured by kinase assays), respectively. Sorafenib inhibited activation of the RAF/MEK/ERK pathway at concentration below 15μM, performing by suppressing p-Erk, in most of cell lines tested (like MDA-MB-231. Mia PaCa 2, HCT 116 and HT-29) independent of which mutation caused aberrant activation of the RAS/RAF pathway. Sorafenib targeted receptor tyrosine kinases and inhibited autophosphorylation of VEGFR-2 and PDGFR-β induced by VEGF165 (30ng/ml) in HUVECs/ NIH 3T3 cells and PDGF BB (10ng/ml) in HAoSMCs, respectively. Oral treatment with Sorafenib, at dose of 7.5-60mg/kg daily for 9 days, illustrated a spectrum of antitumor efficacy in a representative panel of tumor xenograft models in a dose-dependent manner, including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460 and A549. Sorafenib showed significant tumor angiogenesis activity, performing as daily oral administration of 30 or 60 mg/kg Sorafenib produced 50-80% inhibition of microvessel area and microvessel density compared with vehicle group in HT-29 tumors[1].
作用机制 Sorafenib is a multitargeted ATP-competitive inhibitor.[1]

Sorafenib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=7.05989 μM SANGER
A101D Growth Inhibition Assay IC50=21.3752 μM SANGER
A253 Growth Inhibition Assay IC50=34.2296 μM SANGER
A388 Growth Inhibition Assay IC50=1.59165 μM SANGER

Sorafenib 动物研究

Dose Mice: 30 mg/kg, 60 mg/kg[4] (p.o.), 10 mg/kg - 100 mg/kg[2] (p.o.) Woodchucks: 2.5 mg/kg, 5 mg/kg[5] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[6] Rats[6] Dogs[6]
Dose 5 mg/kg (i.v. or p.o.) 5.63 mg/kg (i.v.)
4.85 mg/kg (p.o.)
5.77 mg/kg (i.v.)
5.65 mg/kg (p.o.)
Administration i.v.
p.o.
i.v.
p.o.
i.v.
p.o.
F 78.6% (p.o.) 79.1% (p.o.) 59.9% (p.o.)
AUC0→inf 33.30 mg·h/l (i.v.)
19.54 mg·h/l (p.o.)
T1/2 6.53 h (i.v.)
5.77 h (p.o.)
9.33 h (i.v.)
8.86 h (p.o.)
4.33 h (i.v.)
3.59 h (p.o.)
Tmax 1.0 (p.o.) 1.74 (p.o.) 1.59 (p.o.)
MRT 4.55 h (i.v.)
14.72 h (p.o.)
14.87 h (i.v.)
16.08 h (p.o.)
5.83 h (i.v.)
5.5 h (p.o.)
Vz/F 1.59 L/kg (p.o.) 0.71 L/kg (p.o.)
Cmax 13.17 mg/l (i.v.)
1.15 mg/l (p.o.)
8.35 mg/l (i.v.)
3.65 mg/l (p.o.)
CL 0.15 L/h/kg (i.v.)
0.19 L/h/kg (p.o.)
0.04 L/h/kg (i.v.)
0.06 L/h/kg (p.o.)
0.13 L/h/kg (i.v.)
0.21 L/h/kg (p.o.)
Vz/f 1.09 L/kg (p.o.)
Vss 0.68 L/kg (i.v.) 0.65 L/kg (i.v.) 0.74 L/kg (i.v.)
AUC 24.33 mg·h/l (i.v.)
19.13 mg·h/l (p.o.)
94.16 mg·h/l (i.v.)
64.26 mg·h/l (p.o.)

Sorafenib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03565536 Thyroid Cancer, Anaplastic Phase 2 Recruiting October 30, 2019 China, Fujian ... 展开 >> Fujian Medical University Union Hospital Recruiting FuZhou, Fujian, China, 350001 Contact: bo wang, md    13705947900    wangbo@fjmu.edu.cn 收起 <<
NCT00984425 Solid Tumors Phase 1 Completed - Italy ... 展开 >> Istituto Clinco Humanitas Rozzano, Milano, Italy, 20089 收起 <<
NCT01259193 Hepatocellular Carcinoma Phase 2 Unknown July 2012 China, Shanghai ... 展开 >> Liver Cancer Institute Recruiting Shanghai, Shanghai, China, 200032 Contact: Zheng-Gang Ren, Ph.D    0086-021-64041990 ext 2137    ren.zhenggang@zs-hospital.sh.cn    Contact: Lan Zhang, Master    0086-021-64041990 ext 2171    zhang.lan@zs-hospital.sh.cn    Principal Investigator: Zheng-Gang Ren, Ph.D          Sub-Investigator: Jubo Zhang, PhD 收起 <<

Sorafenib 参考文献

[1]Wilhelm SM, Carter C, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.

[2]Huynh H, Ngo VC, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009;13(8B):2673-83.

[3]El-Ashmawy NE, Khedr EG, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2017;17(2):185-191.

[4]Kuczynski EA, Lee CR, et al. Effects of Sorafenib Dose on Acquired Reversible Resistance and Toxicity in Hepatocellular Carcinoma. Cancer Res. 2015 Jun 15;75(12):2510-9.

[5]Iyer RV, Maguire O, et al. Dose-Dependent Sorafenib-Induced Immunosuppression Is Associated with Aberrant NFAT Activation and Expression of PD-1 in T Cells. Cancers (Basel). 2019 May 16;11(5). pii: E681.

[6]Nexavar

Sorafenib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.51mL

4.30mL

2.15mL

Sorafenib 技术信息

CAS号284461-73-0
分子式C21H16ClF3N4O3
分子量 464.825
别名 Bay 43-9006
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 45 mg/mL(96.81 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

5%DMSO+45%PEG400+50%water 0.375 mg/mL

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