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BBT594 {[allProObj[0].p_purity_real_show]}

货号:A984305 同义名: NVP-BBT594

BBT594 is a potentreceptor tyrosine kinase RET inhibitor, used for cancer treatment.

BBT594 化学结构 CAS号:882405-89-2
BBT594 化学结构
CAS号:882405-89-2
BBT594 3D分子结构
CAS号:882405-89-2
BBT594 化学结构 CAS号:882405-89-2
BBT594 3D分子结构 CAS号:882405-89-2
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BBT594 纯度/质量文件 产品仅供科研

货号:A984305 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 c-RET 其他靶点 纯度
Regorafenib +++

RET, IC50: 1.5 nM

98%
TG101209 ++

RET, IC50: 17 nM

FLT3 99%+
Danusertib +

RET, IC50: 31 nM

99%+
AD80 ++++

RET wt, IC50: 1.3 nM

RET V804M, IC50: 0.6 nM

Src,Raf 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 (ITD), IC50: 1.1 nM

FLT3 (WT), IC50: 4.2 nM

98%
Gilteritinib ++++

FLT3, IC50: 0.29 nM

99%+
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

99%+
Pacritinib ++

FLT3, IC50: 22 nM

FLT3 (D835Y), IC50: 6 nM

97%
Dovitinib ++++

FLT3, IC50: 1 nM

c-Kit 99%+
Denfivontinib ++++

FLT3, IC50: 0.4 nM

FLT3 (D835Y), 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 VEGFR1 VEGFR2 VEGFR3 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

++++

VEGFR2/Flk1, IC50: 3 nM

VEGFR2, 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

++

Flk1, IC50: 25 nM

VEGFR2, 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

c-Kit,FGFR,PDGFR 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

c-Kit,FLT3 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

c-Kit,FLT3 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/Flk1, IC50: 90 nM

VEGFR2, 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

RET,FLT3 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。
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。

BBT594 生物活性

描述 The receptor tyrosine kinase RET (REarranged during Transfection) is activated by its ligand glial-derived neurotrophic factor (GDNF). RET signalling is involved in a diverse range of developmental processes including proliferation, migration survival and/or differentiation[3]. BBT594 is a potent RET inhibitor, used for cancer treatment. In human breast cancer MCF7 cells, BBT594 showed the highest suppression of GDNF-induced RET signaling, as assessed by RET, ERK1/2, AKT and ER phosphorylation, compared with sunitinib and cabozantinib. BBT594 treatment ranging in 0-1000 nM blocked the GDNF-mediated enhancement of MCF7-LTED cell viability in 2D culture and 3D colony formation[4]. 100 nM of BBT594 remarkably elevated the antiproliferative effects of letrozole in MCF7-2A cells[5]. BBT594 also acts as type II JAK inhibitor. BBT594 (1 μM, 48h) alone or combined with rapamycin (0.2 μM)/AZD2014 (0.2 μM) induced modest cell apoptosis in 2 P2RY8-CRLF2 samples (CRLF2-re and JAK2 mutation) and significant cell death in IGH-CRLF2 sample ex vivo[6].

BBT594 参考文献

[1]Andreucci E, Francica P, et al. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Dec 6;7(49):80543-80553.

[2]Morandi A, Martin LA, et al. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95.

[3]Perea D, Guiu J, Hudry B, Konstantinidou C, Milona A, Hadjieconomou D, Carroll T, Hoyer N, Natarajan D, Kallijärvi J, Walker JA, Soba P, Thapar N, Burns AJ, Jensen KB, Miguel-Aliaga I. Ret receptor tyrosine kinase sustains proliferation and tissue maturation in intestinal epithelia. EMBO J. 2017 Oct 16;36(20):3029-3045. doi: 10.15252/embj.201696247. Epub 2017 Sep 12. PMID: 28899900; PMCID: PMC5641678.

[4]Andreucci E, Francica P, Fearns A, Martin LA, Chiarugi P, Isacke CM, Morandi A. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Dec 6;7(49):80543-80553. doi: 10.18632/oncotarget.11826. PMID: 27602955; PMCID: PMC5348339.

[5]Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6. PMID: 23650283; PMCID: PMC3686594.

[6]Zhang Q, Shi C, Han L, Jain N, Roberts KG, Ma H, Cai T, Cavazos A, Tabe Y, Jacamo RO, Mu H, Zhao Y, Wang J, Wu SC, Cao F, Zeng Z, Zhou J, Mi Y, Jabbour EJ, Levine R, Tasian SK, Mullighan CG, Weinstock DM, Fruman DA, Konopleva M. Inhibition of mTORC1/C2 signaling improves anti-leukemia efficacy of JAK/STAT blockade in CRLF2 rearranged and/or JAK driven Philadelphia chromosome-like acute B-cell lymphoblastic leukemia. Oncotarget. 2018 Jan 17;9(8):8027-8041. doi: 10.18632/oncotarget.24261. PMID: 29487712; PMCID: PMC5814279.

BBT594 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.56mL

3.51mL

1.76mL

BBT594 技术信息

CAS号882405-89-2
分子式C28H30F3N7O3
分子量 569.578
别名 NVP-BBT594
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,2-8°C

溶解度

DMSO: 35 mg/mL(61.45 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

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