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Gusacitinib {[allProObj[0].p_purity_real_show]}

货号:A1176575 同义名: ASN-002

Gusacitinib是一种选择性 JAK 抑制剂,能有效抑制 JAK 激酶活性。它在治疗免疫性疾病和某些类型的癌症中展现出潜力。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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+
Gusacitinib 化学结构 CAS号:1425381-60-7
Gusacitinib 化学结构
CAS号:1425381-60-7
Gusacitinib 3D分子结构
CAS号:1425381-60-7
Gusacitinib 化学结构 CAS号:1425381-60-7
Gusacitinib 3D分子结构 CAS号:1425381-60-7
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Gusacitinib 纯度/质量文件 产品仅供科研

货号:A1176575 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 JAK1 JAK2 JAK3 Tyk2 其他靶点 纯度
Decernotinib +++

JAK1, IC50: 11 nM

JAK1, Ki: 11 nM

+++

JAK2, Ki: 13 nM

++++

JAK3, Ki: 2.5 nM

+++

TYK2, Ki: 13 nM

99%+
ZM39923 HCl +

JAK1, pIC50: 4.4

+

JAK3, pIC50: 7.1

EGFR 97%
Cerdulatinib +++

JAK1, IC50: 12 nM

+++

JAK2, IC50: 6 nM

+++

JAK3, IC50: 8 nM

++++

TYK2, IC50: 0.5 nM

99%+
Momelotinib +++

JAK1, IC50: 11 nM

++

JAK2, IC50: 18 nM

+

JAK3, IC50: 155 nM

99%+
XL019 +

JAK1, IC50: 134.3 nM

++++

JAK2, IC50: 2.2 nM

+

JAK3, IC50: 214.2 nM

FLT3 99%+
Ruxolitinib +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

98%
Tofacitinib +

JAK1, IC50: 112 nM

++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

98%
Ruxolitinib (S enantiomer) +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

++

TYK2, IC50: 19 nM

98%
Filgotinib +++

JAK1, IC50: 10 nM

++

JAK2, IC50: 28 nM

+

JAK3, IC50: 810 nM

+

TYK2, IC50: 116 nM

99%
Baricitinib +++

JAK1, IC50: 5.9 nM

+++

JAK2, IC50: 5.7 nM

++

TYK2, IC50: 53 nM

99%
Gandotinib ++

JAK1, IC50: 19.8 nM

++++

JAK2 (V617F), Ki: 0.245 nM

JAK2, IC50: 0.288 nM

++

JAK3, IC50: 48.0 nM

++

TYK2, IC50: 44 nM

FLT3 99%+
Oclacitinib maleate +++

JAK1, IC50: 10nM

++

JAK2, IC50: 18nM

+

JAK3, IC50: 99nM

+

TYK2, IC50: 84nM

98+%
NVP-BSK805 2HCl ++

JAK1, IC50: 31.63 nM

++++

JAK2, IC50: ~0.5 nM

++

JAK3, IC50: 18.68 nM

+++

TYK2, IC50: 10.76 nM

99+%
Peficitinib 98%
Go6976 FLT3 99%+
AZD-1480 ++++

JAK2, IC50: 0.26 nM

99%+
Fedratinib +++

JAK2, IC50: 3 nM

JAK2 (V617F), IC50: 3 nM

FLT3,RET 99%+
WP1066 +

JAK2, IC50: 2.3 μM

98%
Curcumol 98%
AZ960 ++++

JAK2, IC50: <3 nM

JAK2, Ki: 0.45 nM

97%
GLPG0634 analog 99%+
CEP-33779 ++++

JAK2, IC50: 1.8 nM

99%+
FLLL32 +

JAK2, IC50: <5 μM

99%+
WHI-P154 +

JAK3, IC50: 1.8 μM

VEGFR,Src,EGFR 98%
BMS-911543 ++++

JAK2, IC50: 1.1 nM

+

JAK3, IC50: 75 nM

++

TYK2, IC50: 66 nM

98%
TG101209 +++

JAK2, IC50: 6 nM

+

JAK3, IC50: 169 nM

RET,FLT3 99%+
AT9283 ++++

JAK2, IC50: 1.2 nM

++++

JAK3, IC50: 1.1 nM

99%+
Pacritinib ++

JAK2, IC50: 23 nM

JAK2 (V617F), IC50: 19 nM

+

JAK3, IC50: 520 nM

++

TYK2, IC50: 50 nM

FLT3 97%
Tofacitinib citrate ++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

99%
FM-381 ++++

JAK3, IC50: 127 pM

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 Syk 其他靶点 纯度
PRT062607 HCl ++++

Syk, IC50: 1 nM

99%+
R406 ++

Syk, IC50: 41 nM

98%
Fostamatinib Disodium ++

Syk, IC50: 41 nM

99%+
Piceatannol PKC 98%
BAY 61-3606 2HCl +++

Syk, Ki: 7.5 nM

99+%
Entospletinib +++

Syk, IC50: 7.7 nM

99%+
MNS +

Syk, IC50: 2.5 μM

p97,Src 98%
Fostamatinib ++

Syk, IC50: 41 nM

99%+
RO9021 +++

Syk, IC50: 5.6 nM

98%
TAK-659 HCl ++++

Syk, IC50: 3.2 nM

FLT3 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。

Gusacitinib 生物活性

描述 Janus kinase (JAK) and spleen tyrosine kinase (SYK) play critical functions in T-cell activation and in inflammation[1].Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM). Gusacitinib (ASN-002) shows anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types.In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies.Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%) and it also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model [2].

Gusacitinib 参考文献

[1] Ahmad Kheirkhah, Antonio Di Zazzo,et al. A Pilot Randomized Trial on Safety and Efficacy of a Novel Topical Combined Inhibitor of Janus Kinase 1/3 and Spleen Tyrosine Kinase for GVHD-Associated Ocular Surface Disease. Cornea. 2017 Jul;36(7):799-804.

[2]Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April18-22, 2015; Philadelphia, PA.

Gusacitinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.71mL

4.34mL

2.17mL

Gusacitinib 技术信息

CAS号1425381-60-7
分子式C24H28N8O2
分子量 460.531
别名 ASN-002
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,Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(228 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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