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Olverembatinib {[allProObj[0].p_purity_real_show]}

货号:A163539 Ambeed 开学季,买赠积分,赢豪礼

GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50 of 0.34 and 0.68 nM, respectively.

Olverembatinib 化学结构 CAS号:1257628-77-5
Olverembatinib 化学结构
CAS号:1257628-77-5
Olverembatinib 3D分子结构
CAS号:1257628-77-5
Olverembatinib 化学结构 CAS号:1257628-77-5
Olverembatinib 3D分子结构 CAS号:1257628-77-5
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Olverembatinib 纯度/质量文件 产品仅供科研

货号:A163539 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

{[allProObj[0].p_purity_real_show]}
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

{[allProObj[0].p_purity_real_show]}
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

{[allProObj[0].p_purity_real_show]}
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

{[allProObj[0].p_purity_real_show]}
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

{[allProObj[0].p_purity_real_show]}
LDN-214117 ++

ALK2, IC50: 24 nM

{[allProObj[0].p_purity_real_show]}
DMH-1 +

ALK2, IC50: 107.9 nM

{[allProObj[0].p_purity_real_show]}
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

{[allProObj[0].p_purity_real_show]}
Alantolactone {[allProObj[0].p_purity_real_show]}
SIS3 {[allProObj[0].p_purity_real_show]}
Pirfenidone {[allProObj[0].p_purity_real_show]}
Hesperetin {[allProObj[0].p_purity_real_show]}
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
GW788388 +++

ALK5, IC50: 18 nM

{[allProObj[0].p_purity_real_show]}
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

{[allProObj[0].p_purity_real_show]}
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

{[allProObj[0].p_purity_real_show]}
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

{[allProObj[0].p_purity_real_show]}
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

{[allProObj[0].p_purity_real_show]}
Galunisertib ++

TβRI, IC50: 56 nM

{[allProObj[0].p_purity_real_show]}
SB 431542 +

ALK5, IC50: 94 nM

{[allProObj[0].p_purity_real_show]}
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

{[allProObj[0].p_purity_real_show]}
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

FLT3 {[allProObj[0].p_purity_real_show]}
Ponatinib ++++

Abl, IC50: 0.37 nM

{[allProObj[0].p_purity_real_show]}
AT9283 {[allProObj[0].p_purity_real_show]}
Imatinib Mesylate +

v-Abl, IC50: 600 nM

PDGFR,c-Kit {[allProObj[0].p_purity_real_show]}
Danusertib ++

Abl, IC50: 25 nM

RET {[allProObj[0].p_purity_real_show]}
Rebastinib ++++

p-Abl1 (native), IC50: 0.75 nM

u-Abl1 (T315I), IC50: 5 nM

FLT3,Tie-2 {[allProObj[0].p_purity_real_show]}
PP121 ++

Abl, IC50: 18 nM

VEGFR,PDGFR {[allProObj[0].p_purity_real_show]}
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

{[allProObj[0].p_purity_real_show]}
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

{[allProObj[0].p_purity_real_show]}
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

Src {[allProObj[0].p_purity_real_show]}
Dasatinib ++++

Abl, IC50: 0.6 nM

Src {[allProObj[0].p_purity_real_show]}
Bafetinib +++

Abl, IC50: 5.8 nM

{[allProObj[0].p_purity_real_show]}
GNF-2 +

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

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

{[allProObj[0].p_purity_real_show]}
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

DUB {[allProObj[0].p_purity_real_show]}
GNF-5 ++

Bcr-Abl, IC50: 220 nM

{[allProObj[0].p_purity_real_show]}
Radotinib ++

BCR-ABL1, IC50: 34 nM

{[allProObj[0].p_purity_real_show]}
PD173955 Src {[allProObj[0].p_purity_real_show]}
Nilotinib ++

Bcr-Abl, IC50: <30 nM

{[allProObj[0].p_purity_real_show]}
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。

Olverembatinib 生物活性

描述 Bcr-Abl fusion tyrosine kinase is formed because of a reciprocal chromosomal translocation between chromosomes 9 and 22, producing the Philadelphia chromosome. Bcr-Abl is expressed in chronic myeloid leukemia(CML) and a chronic of acute lymphocytic leukemia[3]. GZD824 is an orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including Bcr-AblWT and Bcr-AblT315I with Kd values of 0.32nM and 0.71nM, respectively, and with IC50 values of 0.34nM and 0.68nM, respectively. In vitro, GZD824 potently suppressed proliferation of Bcr-Abl positive human CML cell lines K562 , Ku812, SUP-B15, U-937, MOLT4 and HL-60 with IC50 values of 0.2nM, 0.13nM, 2.5nM, 390.2nM, 26.3nM, and348.9nM, respectively. GZD824 suppressed the activation of Bcr-Abl and downstream Crk1 and STAT5 in a dose-dependent manner in K562 cells. In vivo, oral administration of GZD824 at 5 and 10mg/kg once daily for 14 consecutive days significantly suppressed tumor growth in mice bearing xenografted K562 cells. Oral administration of GZD824 at 1mg/kg once daily for 14 days induced complete tumor regression in mice bearing xenografted Ku812 cells. In addition, treatment of the mice bearing xenografted Ba/F3 cells expressing Bcr-Abl T315I with GZD824 at dose of 20mg/kg once daily via oral administration for 14 days induced almost complete tumor regression[1].
作用机制 GZD824 inhibits the activation of Bcr-Abl by binding to the ATP-binding site of nonphosphorylated(DGF-out) Bcr-Abl[1].

Olverembatinib 动物研究

Dose Mice: 25 mg/kg[2] (i.g.) Rat: 25 mg/kg[1] (p.o.); 5 mg/kg[1] (i.v.)
Administration i.g., p.o., i.v.
Pharmacokinetics
Animal Rats[1]
Dose 5 mg/kg (i.v.)
25 mg/kg (p.o.)
Administration i.v.
p.o.
MRT 6.7 h (i.v.)
17.9 h (p.o.)
F 48.7% (p.o.)
T1/2 5.6 h (i.v.)
10.6 h (p.o.)
Tmax 0.067 h (i.v.)
4.0 h (p.o.)
CL 1.7 L/h/kg (i.v.)
3.6 L/h/kg (p.o.)
Cmax 1375.6 μg/L (i.v.)
390.5 μg/L (p.o.)
AUC0→∞ 2922.4 μg·h/L (i.v.)
7108.2 μg·h/L (p.o.)
Vss 13.7 L/h/kg (i.v.)
53.2 L/h/kg (p.o.)
AUC0→t 2737.3 μg·h/L (i.v.)
6699.0 μg·h/L (p.o.)

Olverembatinib 参考文献

[1]Ren X, Pan X, Zhang Z, et al. Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. Journal of Medicinal Chemistry, 2013, 56(3): 879-894

[2]Ye W, Jiang Z, et al. GZD824 suppresses the growth of human B cell precursor acute lymphoblastic leukemia cells by inhibiting the SRC kinase and PI3K/AKT pathways. Oncotarget. 2016 Jul 28;8(50):87002-87015.

[3]Skorski T. BCR-ABL1 Kinase: Hunting an Elusive Target with New Weapons. Chemistry & Biology, 2011, 18(11): 1352-1353

Olverembatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

Olverembatinib 技术信息

CAS号1257628-77-5
分子式C29H27F3N6O
分子量 532.559
别名
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 40 mg/mL(75.11 mM),配合低频超声,并水浴加热至45℃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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