3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine
LY2784544
CAS: 1229236-86-5
Molecular Formula: C23H25ClFN7O
3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine - Names and Identifiers
3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine - Physico-chemical Properties
| Molecular Formula | C23H25ClFN7O |
| Molar Mass | 469.94 |
| Density | 1.45 |
| Solubility | DMSO 94 mg/mL (200.02 mM); Water <1 mg/mL (<1 mM); Ethanol 9 mg/mL (19.15 mM) |
| pKa | 14.12±0.10(Predicted) |
| Storage Condition | -20℃ |
| MDL | MFCD20482143 |
| Use | A selective inhibitor of JAK2 mutant V617F. |
| In vitro study | LY2784544 also inhibited IL-3-activated wild-type JAK2 with an IC50 of 2.26 µm. In the proliferation experiment, LY2784544 has anti-proliferative activity with an IC50 of 68 nM in cells driven by JAK2 V617F, while it has an IC50 of 1356 nM in cells driven by wild-type JAK2, when acting on jak3-driven cells, the IC50 was 940 nM. |
| In vivo study | LY2784544 significantly inhibited STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a threshold effective dose 50 (TED50) of 12.7 mg/kg. LY2784544 acts on the MPN model induced by JAK2 V617F and also reduces the tumor burden V617F-GFP Ba/F3-JAK2, with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 was orally applied to the spleen of SCID mice and had no effect on CD71/Ter119 positive erythroid progenitor cells. |
3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine - Introduction
LY2784544 is an effective JAK2 inhibitor with IC50 of 3 nM, which is effective on JAK2V617F and has 8 and 20 times higher selectivity than on JAK1 and JAK3. Phase 2.
Last Update：2022-10-16 17:41:22
3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine - Reference Information
| introduction | Gandotinib (LY2784544) is an effective JAK2 inhibitor with IC50 of 3nM, effective on JAK2 V617F, 8 and 20 times higher selectivity than on JAK1 and JAK3. |
| biological activity | Gandotinib (LY2784544) is an effective JAK2 inhibitor with IC50 of 3 nM, which is effective on JAK2V617F and has 8 and 20 times higher selectivity than on JAK1 and JAK3. Phase 2. |
| Target | Value |
| JAK2 (V617F) | 0.245 nM(Ki) |
| JAK2 | 0.288 nM(Ki) |
| JAK2 (Cell-free assay) | 3 nM |
| FLT3 | 4 nM |
| JAK1 | 19.8 nM |
Last Update：2024-04-09 21:54:55
![3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine](http://res.chembk.com/assets/str/2d/1/12/1229236-86-5.png)
Supplier List
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
Spot supply
Product Name: Gandotinib Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: LY2784544 Visit Supplier Webpage Request for quotation
CAS: 1229236-86-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1229236-86-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
Spot supply
Product Name: Gandotinib Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: LY2784544 Visit Supplier Webpage Request for quotationCAS: 1229236-86-5
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: LY2784544 Visit Supplier Webpage Request for quotation
CAS: 1229236-86-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1229236-86-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine
2-[2-(4-chlorophenoxy)-2-methylpropanoyl]oxyethyl pyridin-1-ium-3-carboxylate
Dl-alanine, 3-(p-[bis(2-chloroethyl)amino]phenyl)-, hydrochloride
2-(4-(叔丁氧基羰基)哌嗪-1-基)-2-甲基丙酸
1-[2-Bromoethenyl]-4-(trifluoromethyl)benzene E/Z-mixture
3-ETHYL-9-METHYL-3,9-DIAZABICYCLO[3.3.1]NONAN-6-ONE
4-氯-6-丙基氨基嘧啶
2-CHLORO-3-(2,4-DICHLOROPHENYL)PROPANENITRILE, TECH
Imidazo[1,2-a]pyridin-2-ol, 5,6,7,8-tetrahydro-
4-三氟甲基-1H-吡咯-2-甲酸甲酯
2-[2-(4-chlorophenoxy)-2-methylpropanoyl]oxyethyl pyridin-1-ium-3-carboxylate
Dl-alanine, 3-(p-[bis(2-chloroethyl)amino]phenyl)-, hydrochloride
2-(4-(叔丁氧基羰基)哌嗪-1-基)-2-甲基丙酸
1-[2-Bromoethenyl]-4-(trifluoromethyl)benzene E/Z-mixture
3-ETHYL-9-METHYL-3,9-DIAZABICYCLO[3.3.1]NONAN-6-ONE
4-氯-6-丙基氨基嘧啶
2-CHLORO-3-(2,4-DICHLOROPHENYL)PROPANENITRILE, TECH
Imidazo[1,2-a]pyridin-2-ol, 5,6,7,8-tetrahydro-
4-三氟甲基-1H-吡咯-2-甲酸甲酯