GNF-7 | BCR-ABL Inhibitor | AmBeed-信号通路专用抑制剂

GNF-7 {[allProObj[0].p_purity_real_show]}

货号：A472268

GNF-7是一种多重激酶抑制剂，能够抑制 Bcr-Abl WT 和 Bcr-Abl T315I，IC50分别为 133 nM 和 61 nM。此外，它还抑制 ACK1 和 GCK，IC50值分别为 25 nM 和 8 nM。

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

GNF-7 化学结构
CAS号：839706-07-9

GNF-7 3D分子结构
CAS号：839706-07-9

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GNF-7 质控信息

转化生长因子-β 亚型比较

Bcr-Abl 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	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 2HCl	++++ 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%
(E/Z)-SIS3 free base						✔				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		99%
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, IC50: 14 nM Abl (T315I), IC50: 4 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	++++ p-Abl1 (native), IC50: 0.75 nM u-Abl1 (T315I), IC50: 5 nM		Tie-2,FLT3	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ M351T, IC50: 133 nM E255V, IC50: 122 nM			99%+
Olverembatinib dimesylate	++++ Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 nM			98%
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 (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB/Deubiquitinase	99+%
GNF-5		++ Bcr-Abl, IC50: 220 nM		99%
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。

GNF-7 生物活性

靶点

Abl

M351T, IC50:133 nM

E255V, IC50:122 nM

描述

The BCR-ABL oncogene is generated by the Philadelphia chromosome (Ph) translocation, fusing the BCR gene to the ABL gene. The BCR-ABL fusion protein has elevated ABL tyrosine kinase activity that is critical for transformation of hematopoietic cells^[3]. GNF-7 is a multikinase inhibitor. It is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies^[4].GNF-7 inhibited necroptosis in both human and mouse cells, while not protecting cells from apoptosis. Drug affinity responsive target stability assay (DARTS) demonstrated that it binds with RIPK1 and RIPK3. GNF-7 inhibited RIPK1 and RIPK3 kinase activities and thus disrupted RIPK1-RIPK3 necrosome complex formation. In vivo, GNF-7 ameliorated both cisplatin- and ischemia/reperfusion-induced AKI. Orally administration of GNF-7 attenuated renal cell necrosis and reduced pro-inflammatory responses in mouse models of AKI^[5]. GNF-7 potently inhibits wild-type Bcr-Abl (IC50<5 nM) and Bcr-Abl mutants such as T315I (IC50=11 nM), G250E (IC50<5 nM), E255V (IC50=10 nM), F317L (IC50<5 nM) and M351T (IC50<5 nM) in cellular assays. GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg).GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)^[6].

GNF-7 细胞实验

Cell Line Hela cells OCI-AML3 (NRAS-Q61L) HT-29 (KRAS-Q61L) MDA-MB-231 (KRAS-G13D) SW480 (KRAS-G12V) DU-145 (KRAS-G12V) AsPC-1 (KRAS-G12D) H358 (KRAS-G12C) Ba/F3 cells (NRAS-G12V transformed) Ba/F3 cells (NRAS-G12D transformed) WM3629 WM3670 C8161 A375 SK-MEL-28 SK-MEL-2 HEK293T SW620 Colo205 Ba/F3-T315I-Bcr-Abl	Concentration	Treated Time	Description	References
Hela cells	50 µM	2 days	GNF-7 treatment reduced miR-21-5p levels to ~35% compared to the controls.	Sci Rep. 2023 Mar 31;13(1):5244.
OCI-AML3 (NRAS-Q61L)	0.229 ± 0.010 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited NRAS-Q61L mutated OCI-AML3 cells	Front Oncol. 2021 Dec 9;11:768022.
HT-29 (KRAS-Q61L)	0.938 ± 0.034 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-Q61L mutated HT-29 cells	Front Oncol. 2021 Dec 9;11:768022.
MDA-MB-231 (KRAS-G13D)	0.296 ± 0.039 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-G13D mutated MDA-MB-231 cells	Front Oncol. 2021 Dec 9;11:768022.
SW480 (KRAS-G12V)	0.760 ± 0.063 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-G12V mutated SW480 cells	Front Oncol. 2021 Dec 9;11:768022.
DU-145 (KRAS-G12V)	0.288 ± 0.057 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-G12V mutated DU-145 cells	Front Oncol. 2021 Dec 9;11:768022.
AsPC-1 (KRAS-G12D)	0.448 ± 0.027 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-G12D mutated AsPC-1 cells	Front Oncol. 2021 Dec 9;11:768022.
H358 (KRAS-G12C)	0.922 ± 0.093 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited KRAS-G12C mutated H358 cells	Front Oncol. 2021 Dec 9;11:768022.
Ba/F3 cells (NRAS-G12V transformed)	0.396 ± 0.036 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited NRAS-G12V transformed Ba/F3 cells	Front Oncol. 2021 Dec 9;11:768022.
Ba/F3 cells (NRAS-G12D transformed)	0.250 ± 0.026 (GI50 )	72 hours	Evaluate anti-proliferative activity, results showed GNF-7 inhibited NRAS-G12D transformed Ba/F3 cells	Front Oncol. 2021 Dec 9;11:768022.
WM3629	0.21 ± 0.00 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on WM3629 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
WM3670	0.13 ± 0.01 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on WM3670 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
C8161	0.02 ± 0.00 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on C8161 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
A375	0.06 ± 0.00 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on A375 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
SK-MEL-28	0.15 ± 0.02 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on SK-MEL-28 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
SK-MEL-2	0.23 ± 0.08 µM (GI50 )	72 hours	Evaluate anti-proliferative activity, GNF-7 showed anti-proliferative activity on SK-MEL-2 cells	Int J Mol Sci. 2021 Apr 6;22(7):3783.
HEK293T	>10 µM		To evaluate the growth inhibitory activity of GNF-7 against non-cancer cells	J Med Chem. 2010 Aug 12;53(15):5439-48.
SW620	0.001 µM		To evaluate the growth inhibitory activity of GNF-7 against colon cancer cells	J Med Chem. 2010 Aug 12;53(15):5439-48.
Colo205	0.005 µM		To evaluate the growth inhibitory activity of GNF-7 against colon cancer cells	J Med Chem. 2010 Aug 12;53(15):5439-48.
Ba/F3-T315I-Bcr-Abl	11 nM		To evaluate the antiproliferative activity of GNF-7 against T315I Bcr-Abl mutant cells	J Med Chem. 2010 Aug 12;53(15):5439-48.

Cell Line

Concentration

Treated Time

Description

References

Hela cells

50 µM

2 days

GNF-7 treatment reduced miR-21-5p levels to ~35% compared to the controls.

Sci Rep. 2023 Mar 31;13(1):5244.

OCI-AML3 (NRAS-Q61L)

0.229 ± 0.010 µM (GI50 )

72 hours

Evaluate anti-proliferative activity, results showed GNF-7 inhibited NRAS-Q61L mutated OCI-AML3 cells