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AG-490

Catalog No. A10047
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EGFR 抑制剂

AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。了解更多

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- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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AZ-960

Catalog No. A10104
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JAK2抑制剂

AZ-960是一种有效的，选择性的和ATP竞争性的JAK2抑制剂，在体外抑制JAK2激酶的Ki为0.45 nM，并诱导成年T细胞白血病（ATL）细胞的生长停滞和凋亡了解更多

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Go 6976

Catalog No. A12419
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PKC 抑制剂

Go6976是一种有效的PKC抑制剂，对PKC（大鼠脑），PKCα和PKCβ1的IC50分别为7.9 nM，2.3 nM和6.2 nM。也是JAK2和Flt3的有效抑制剂。了解更多

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AT9283

Catalog No. A10095
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Aurora/JAK 抑制剂

AT9283抑制极光激酶A和B，并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。了解更多

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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
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Curcumol

Catalog No. A10247
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JAK2 抑制剂

Curcumol是常见的传统中药，具有抗肿瘤活性。了解更多

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Baricitinib (LY3009104)

Catalog No. A11329
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JAK 抑制剂

Baricitinib，也称为INCB028050或LY3009104，是一种选择性口服可生物利用的JAK1/JAK2抑制剂，对JAK1（5.9 nM）和JAK2（5.7 nM）具有纳摩尔浓度。了解更多

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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Yutian Lei, .et al. A multicenter blinded preclinical randomized controlled trial on Jak1/2 inhibition in MRL/MpJ-Fas lpr mice with proliferative lupus nephritis predicts low effect size, Kidney Int, 2021, Feb 16 PMID: 33607177
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XL019

Catalog No. A12394
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JAK2 抑制剂

XL019是janus相关激酶2 (JAK-2)的生物可利用抑制剂，具有潜在的抗肿瘤活性。了解更多

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INCB018424 (Ruxolitinib)

Catalog No. A11041
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JAK1/2 抑制剂

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. IL6/STAT3 Signaling Hijacks Estrogen Receptor α Enhancers to Drive Breast Cancer Metastasis, Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. JAK2V617F+ myeloproliferative neoplasm clones evoke paracrine DNA damage to adjacent normal cells through secretion of lipocalin-2., Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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Cyt387 (Momelotinib)

Catalog No. A10263
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JAK 抑制剂

Cyt387 (Momelotinib)是Janus激酶JAK1和JAK2的抑制剂，可作为ATP竞争者，IC50值分别为11和18 nM。了解更多

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- Alex Bainbridge, .et al. IKBKE activity enhances AR levels in advanced prostate cancer via modulation of the Hippo pathway, Nucleic Acids Research, 2020, April
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TG101209

Catalog No. A11180
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JAK2 抑制剂

TG101209是一种新型的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性，并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。了解更多

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Pacritinib (SB1518)

Catalog No. A12694
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JAK2/FLT3 抑制剂

Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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LY2784544 (Gandotinib)

Catalog No. A10546
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JAK 抑制剂

LY2784544被鉴定为对JAK2-V617F具有高度选择性，并已进入人类临床试验，用于治疗几种骨髓增生性疾病。了解更多

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TG-101348 (Fedratinib, SAR302503)

Catalog No. A11082
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JAK2/FLT3 抑制剂

TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。了解更多

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WP1066

Catalog No. A11795
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JAK 抑制剂

WP1066是一种新型的JAK2抑制剂，可抑制携带JAK2 V617F突变的类人甲状腺细胞增殖并诱导其凋亡。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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AZD1480

Catalog No. A10110
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JAK 抑制剂

AZD1480是一种新型有效的小型JAK2抑制剂，IC50为0.26 nM。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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NVP-BSK805

Catalog No. A11193
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JAK 抑制剂

NVP-BSK805是喹喔啉JAK2抑制剂对红细胞增多症的有效和选择性抑制，喹喔啉JAK2抑制剂可有效抑制小鼠和大鼠中重组人促红细胞生成素诱导的红细胞增多症和髓外红细胞生成。IC50为0.5 nM，比作用于JAK1， JAK3和TYK2选择性高20倍以上。了解更多

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CEP33779

Catalog No. A12808
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JAK2 抑制剂

CEP33779是选择性JAK2抑制剂，IC50为1.8 nM。了解更多

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