945755-56-6
XL019
CAS: 945755-56-6
Molecular Formula: C25H28N6O2
945755-56-6 - Names and Identifiers
945755-56-6 - Physico-chemical Properties
| Molecular Formula | C25H28N6O2 |
| Molar Mass | 444.53 |
| Solubility | Soluble in DMSO, not in water |
| Storage Condition | -20℃ |
| Use | XL019 is an effective, orally active and selective JAK2 inhibitor. The IC50 for JAK2,JAK1 and JAK3 is 2.2, 134.3 and 214.2 nM respectively. The selectivity of XL019 for JAK2 is 50 times or higher than that of more 100 serine/threonine and tyrosine kinases (including other members of the JAK family). Inhibitory effect of XL019 on STAT3 and STAT5 phosphorylation in JAK2 V617F and wild-type JAK2 cells. |
| In vitro study | XL019 is a highly selective inhibitor of JAK2, binding to the active site of JAK2 with 50-fold selectivity over JAK1 and tyk2. XL019 exhibited ideal inhibition of CYP(1A2,2C9,2D6,3A4> 20 μm),hERG(16 μm), and P-glycoprotein (> 20 μm). XL019 inhibits activation of JAK2 as well as the mutant form of JAK2V617F, which may lead to JAK-STAT inhibition of the signaling pathway and may induce apoptosis. XL019 showed more than 10-fold selective inhibition in erythroid cells compared to other cellular systems (IC 50=64 nM). XL019 is a highly selective inhibitor of JAK2, binding to the active site of JAK2 with 50-fold selectivity over JAK1 and tyk2. XL019 exhibited ideal inhibition of CYP(1A2,2C9,2D6,3A4> 20 μm),hERG(16 μm), and P-glycoprotein (> 20 μm). XL019 inhibits activation of JAK2 as well as the mutant form of JAK2V617F, which may lead to JAK-STAT inhibition of the signaling pathway and may induce apoptosis. XL019 showed more than 10-fold selective inhibition in erythroid cells compared to other cellular systems (IC 50=64 nM). |
| In vivo study | After administration of 30,100, and 300 mg/kg, XL019 significantly inhibited the downstream markers pSTAT1 and pSTAT3, resulting in an ED 50 of 42 mg/kg, respectively (pSTAT1). And 210 mg/kg (pSTAT3). XL019 has superior efficacy and good oral absorption, and shows moderate clearance and half-life in different species. In mice, XL019 inhibited HEL.92.1.7 xenograft tumor growth with 200 mg / kg and 300 mg / kg administered twice daily for up to 14 days showing 60% and 70% inhibition, respectively. The 300 mg/kg dose exhibited a 11.3-fold increase in apoptosis compared to the control. after administration of 30,100, and 300 mg/kg, XL019 significantly inhibited the downstream markers pSTAT1 and pSTAT3, resulting in an ED 50 of 42 mg/kg (pSTAT1), respectively. And 210 mg/kg (pSTAT3). XL019 has superior efficacy and good oral absorption, and shows moderate clearance and half-life in different species. In mice, XL019 inhibited HEL.92.1.7 xenograft tumor growth with 200 mg / kg and 300 mg / kg administered twice daily for up to 14 days showing 60% and 70% inhibition, respectively. The 300 mg/kg dose exhibited a 11.3-fold increase in apoptosis compared to the control. |
945755-56-6 - Reference
| Reference Show more | 1: Verstovsek S, Tam CS, Wadleigh M, Sokol L, Smith CC, Bui LA, Song C, Clary DO, Olszynski P, Cortes J, Kantarjian H, Shah NP. Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor. Leuk Res. 2013 Dec 11. pii: S0145-2126(13)00425-6. doi: 10.1016/j.leukres.2013.12.006. [Epub ahead of print。 |
945755-56-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.25 ml | 11.248 ml | 22.496 ml |
| 5 mM | 0.45 ml | 2.25 ml | 4.499 ml |
| 10 mM | 0.225 ml | 1.125 ml | 2.25 ml |
| 5 mM | 0.045 ml | 0.225 ml | 0.45 ml |
Last Update：2024-01-02 23:10:35
945755-56-6 - Reference Information
| biological activity | XL019 is an effective and selective JAK2 inhibitor with IC50 of 2.2 nM, which acts on JAK1, JAK3 and TYK2. The selectivity is 50 times higher. Phase 1. XL019 is an effective and selective JAK2 inhibitor, IC50 is 2.2 nM, which acts on JAK1, JAK3 and TYK2. The selectivity is 50 times higher. Phase 1. |
| in vitro study | XL019 is a highly selective JAK2 inhibitor, which binds to the active site of JAK2 and is 50 times more selective than JAK1 and TYK2. XL019 showed ideal inhibition of CYP(1A2,2C9,2D6,3A4 ≥ 20 μM),hERG(16 μM), and P-glycoprotein (> 20 μM). XL019 inhibits the activation of JAK2 and JAK2V617F of mutant forms, which may lead to the inhibition of JAK-STAT signal transduction pathways and can induce apoptosis. Compared with other cell systems, XL019 showed more than 10-fold selective inhibition in erythroid cells (IC 50=64 nM). XL019 is a highly selective inhibitor of JAK2, which binds to the active site of JAK2, and the selectivity is 50 times that of JAK1 and TYK2. XL019 showed ideal inhibition of CYP(1A2,2C9,2D6,3A4 ≥ 20 μM),hERG(16 μM), and P-glycoprotein (> 20 μM). XL019 inhibits the activation of JAK2 and JAK2V617F of mutant forms, which may lead to the inhibition of JAK-STAT signal transduction pathways and can induce apoptosis. Compared with other cell systems, XL019 showed more than 10-fold selective inhibition in erythroid cells (IC 50=64 nM). |
| in vivo study | after administration of 30,100, and 300 mg/kg, XL019 significantly inhibited the downstream markers pSTAT1 and pSTAT3, resulting in ED 50 of 42 mg/kg (pSTAT1) and 210 mg/kg (pSTAT3), respectively. XL019 has superior efficacy and good oral absorption, showing moderate clearance and half-life in different species. In mice, XL019 inhibits HEL. 92.1.7 xenograft tumor growth, 200 mg/kg and 300 mg/kg were administered twice daily until 14 days, showing 60% and 70% inhibition. Compared with the control, the dose of 300 mg/kg showed a 11.3-fold increase in apoptosis. after administration of 30,100, and 300 mg/kg, XL019 significantly inhibited the downstream markers pSTAT1 and pSTAT3, resulting in ED 50 of 42 mg/kg (pSTAT1) and 210 mg/kg (pSTAT3), respectively. XL019 has superior efficacy and good oral absorption, showing moderate clearance and half-life in different species. In mice, XL019 inhibits HEL. 92.1.7 xenograft tumor growth, 200 mg/kg and 300 mg/kg were administered twice daily until 14 days, showing 60% and 70% inhibition. Compared with the control, the dose of 300 mg/kg showed a 11.3-fold increase in apoptosis. |
| features | Orally bioavailable JAK2-selective inhibitor and has been testing in Phase I clinical trials for treatment of Myelofibrosis. |
| target | TargetValue JAK2 (Cell-free assay) 2.2 nM PDGFRβ (Cell-free assay) 125.4 nM JAK1 (Cell-free assay) 134.3 nM FLT3 (Cell-free assay) 139.7 nM JAK3 (Cell-free assay) 214.2 nM |
| Target | Value |
| JAK2 (Cell-free assay) | 2.2 nM |
| PDGFRβ (Cell-free assay) | 125.4 nM |
| JAK1 (Cell-free assay) | 134.3 nM |
| FLT3 (Cell-free assay) | 139.7 nM |
| JAK3 (Cell-free assay) | 214.2 nM |
Last Update：2024-04-09 21:04:16
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Product Name: XL019 Visit Supplier Webpage Request for quotationCAS: 945755-56-6
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: XL019 Request for quotationCAS: 945755-56-6
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: XL019 Visit Supplier Webpage Request for quotationCAS: 945755-56-6
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: XL019 Visit Supplier Webpage Request for quotationCAS: 945755-56-6
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: XL019 Visit Supplier Webpage Request for quotationCAS: 945755-56-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
945755-56-6
CHEMBRDG-BB 5469887
大麦芽碱硫酸盐
EPA Pesticide Chemical Code 013505
二叔丁基苯膦
壳聚糖季铵盐价格
二氯异三聚氰酸钠盐
硫酸奎尼丁二水物
2703756-54-9
磷酸酯叔胺盐
CHEMBRDG-BB 5469887
大麦芽碱硫酸盐
EPA Pesticide Chemical Code 013505
二叔丁基苯膦
壳聚糖季铵盐价格
二氯异三聚氰酸钠盐
硫酸奎尼丁二水物
2703756-54-9
磷酸酯叔胺盐