Bosutinib hydrate | SKI-606 hydrate | Src/Abl tyrosine kinase inhibitor

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Bosutinib hydrate {[allProObj[0].p_purity_real_show]}

货号：A333356 同义名： SKI-606 hydrate

Bosutinib hydrate是一种口服有效的 Src/Abl 酪氨酸激酶抑制剂，IC₅₀ 值分别为 1.2 nM 和 1 nM，广泛用于研究与 Src/Abl 相关的信号通路和癌症治疗。

Bosutinib hydrate 化学结构
CAS号：918639-08-4

Bosutinib hydrate 3D分子结构
CAS号：918639-08-4

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Bosutinib hydrate 纯度/质量文件产品仅供科研

货号：A333356 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Src 亚型比较
Bcr-Abl 亚型比较
转化生长因子-β 亚型比较

产品名称	Fyn ↓ ↑	Lck ↓ ↑	Lyn ↓ ↑	Src ↓ ↑	Yes ↓ ↑	其他靶点	纯度
Saracatinib	++ Fyn, IC50: 10 nM	++++ LCK, IC50: <4 nM	+++ Lyn, IC50: 5 nM	++++ c-Src, IC50: 2.7 nM			99%+
SU6656	+ Fyn, IC50: 170 nM		+ Lyn, IC50: 130 nM	+ Src, IC50: 280 nM	++ YES, IC50: 20 nM		98%
PP1	+++ Fyn, IC50: 6 nM	+++ LCK, IC50: 5 nM				EGFR	99%+
PP2	+++ Fyn, IC50: 5 nM	++++ LCK, IC50: 4 nM					98%
WH-4-023		++++ Lck, IC50: 2 nM		+++ Src, IC50: 6 nM			99%+
NVP-BHG 712				+ c-Src, IC50: 1.266 μM			99%+
CCT196969		++ LCK, IC50: 0.02 μM		+ Src, IC50: 0.03 μM			98%
MNS				+ Src, IC50: 29.3 μM		Syk,p97	98%
Tirbanibulin				++ Src (Hep 3B), GI50: 26 nM Src (HuH7), GI50: 13 nM			99%+
PP121				++ Src, IC50: 14 nM		VEGFR,PDGFR	99%+
Bosutinib				++++ Src, IC50: 1.2 nM			99%
Dasatinib monohydrate				++++ Src, IC50: 0.8 nM			98%
Quercetin				✔		Sirtuin,PKC	97%
Dasatinib				++++ Src, IC50: 0.8 nM			98%
Repotrectinib				+++ Src, IC50: 5.3 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		VEGFR,PDGFR	99%+
GNF-7	+++ M351T, IC50: 133 nM E255V, IC50: 122 nM			99%+
Olverembatinib dimesylate	++++ Abl, IC50: 0.34 nM Abl (G250E), IC50: 0.35 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	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 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。

Bosutinib hydrate 生物活性

描述

Bosutinib hydrate is an orally active inhibitor of Src/Abl tyrosine kinases, with IC50 values of 1.2 nM and 1 nM, respectively^[1]. Bosutinib hydrate is an active inhibitor of Bcr-Abl across various chronic myelogenous leukemia cell lines, with IC50 values within the low nanomolar range^[2]. Treatment with Bosutinib hydrate for 72 hours in KCL22, K562, KU812, and Lama84 cells inhibits a variety of human CML-derived cell lines, with IC50 values ranging from 1 to 20 nM^[2].

Bosutinib hydrate 动物研究

Animal study

Bosutinib hydrate, administered via oral gavage at 75 mg/kg twice daily or 150 mg/kg once daily, is active against human KU812 xenografts in nude mice. Additionally, Bosutinib hydrate at 150 mg/kg once daily for 5 days a week is effective against both wild-type Bcr-Abl and mutant Ba/F3 xenografts^[2].

Bosutinib hydrate 参考文献

[1]Jorge E Cortes, et al. Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial. J Clin Oncol. 2012 Oct 1;30(28):3486-92.

[2]Miriam Puttini, et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res. 2006 Dec 1;66(23):11314-22.

Bosutinib hydrate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.82mL

0.36mL

0.18mL

9.12mL

1.82mL

0.91mL

18.23mL

3.65mL

1.82mL

Bosutinib hydrate 技术信息

CAS号	918639-08-4
分子式	C₂₆H₃₁Cl₂N₅O₄
分子量	548.461

别名	SKI-606 hydrate
运输	蓝冰

存储条件	液体 -20°C:3-6个月-80°C:12个月
溶解度	DMSO: 105 mg/mL(191.44 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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