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NVP-BHG 712 {[allProObj[0].p_purity_real_show]}

货号:A219560 同义名: BHG712

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition and also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.

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Type HazMat fee for 500 gram (Estimated)
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Limited Quantity USD 15-60
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NVP-BHG 712 化学结构 CAS号:940310-85-0
NVP-BHG 712 化学结构
CAS号:940310-85-0
NVP-BHG 712 3D分子结构
CAS号:940310-85-0
NVP-BHG 712 化学结构 CAS号:940310-85-0
NVP-BHG 712 3D分子结构 CAS号:940310-85-0
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NVP-BHG 712 纯度/质量文件 产品仅供科研

货号:A219560 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

99%+
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

98%
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%
LDN-214117 ++

ALK2, IC50: 24 nM

98%
DMH-1 +

ALK2, IC50: 107.9 nM

99%+
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

99%+
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

99%+
Alantolactone 98%
SIS3 97%
Pirfenidone 98%
Hesperetin 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

98%
GW788388 +++

ALK5, IC50: 18 nM

98%
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

98%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

99%+
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

99%+
Galunisertib ++

TβRI, IC50: 56 nM

98%
SB 431542 +

ALK5, IC50: 94 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 Abl Bcr-Abl 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

99%+
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

Tie-2,FLT3 99%+
PP121 ++

Abl, IC50: 18 nM

PDGFR,VEGFR 99%+
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

99%+
Olverembatinib dimesylate ++++

Abl (G250E), IC50: 0.35 nM

Abl, IC50: 0.34 nM

99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

98+%
GNF-2 +

Bcr-Abl (K562 cell line), IC50: 273 nM

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

98%
Radotinib ++

BCR-ABL1, IC50: 34 nM

98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

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 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 WT, IC50: 32 nM

BRAF(V600E), IC50: 23 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 WT, IC50: 15 nM

BRAF(V600E), IC50: 5.8 nM

++++

C-Raf, IC50: 4.3 nM

99%+
Agerafenib ++

B-Raf (V600E), Kd: 14 nM

B-Raf, Kd: 36 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, IC50: 22 nM

B-Raf (V599E), IC50: 38 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。

NVP-BHG 712 生物活性

靶点
  • Src

    c-Src, IC50:1.266 μM

  • Abl

    c-Abl, IC50:1.667 μM

  • C-Raf/Raf-1

    C-Raf, IC50:0.395 μM

描述 NVP-BHG712 is an orally active inhibitor of EphB4 kinase autophosphorylation, with IC50 values of 3.3 nM for EphA2 and 3.0 nM for EphB4[1][2].
体内研究

NVP-BHG712, administered orally at doses of 3, 10, and 30 mg/kg daily, inhibits VEGF-driven tissue growth and angiogenesis[2].

体外研究

NVP-BHG712 inhibits VEGF-driven vessel formation but has minimal effects on VEGF receptor (VEGFR) activity. This indicates significant crosstalk between VEGFR and EphR signaling during vessel formation[2].

NVP-BHG 712 参考文献

[1]Tröster A, et al. NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. ChemMedChem. 2018 Aug 20;13(16):1629-1633.

[2]Martiny-Baron G, et al. The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Angiogenesis. 2010 Sep;13(3):259-67.

NVP-BHG 712 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL

NVP-BHG 712 技术信息

CAS号940310-85-0
分子式C26H20F3N7O
分子量 503.478
别名 BHG712
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 30 mg/mL(59.59 mM),配合低频超声助溶,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
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