Gandotinib (LY2784544)
LY2784544
CAS: 1229236-86-5
Molecular Formula: C23H25ClFN7O
Gandotinib (LY2784544) - Names and Identifiers
Gandotinib (LY2784544) - 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. |
Gandotinib (LY2784544) - 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
Gandotinib (LY2784544) - 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
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View History
Gandotinib (LY2784544)
2-Pentene-1,4-diol, 5-chloro-4-(2,4-dichlorophenyl)-, (Z)- (9CI)
(R)-2,6-dioxohexahydropyrimidine-4-carboxylic acid
L-Leucine, N-[N-[N-[N-[N-[(1,1-dimethylethoxy)carbonyl]-L-tyrosyl]-O-(1,1-dimethylethyl)-D-seryl]glycyl]-L-phenylalanyl]- (9CI)
PAM BOC-L-THREONINE (BZL)
京尼平甙酸
CUPRESSUFLAVONE WITH HPLC
3-(4-FLUOROPHENYL)PROPRIONIC ACID
AMINO-(3-CHLORO-4-METHOXY-PHENYL)-ACETIC ACID
3-氨基-5-羟基吡啶二盐酸盐
2-Pentene-1,4-diol, 5-chloro-4-(2,4-dichlorophenyl)-, (Z)- (9CI)
(R)-2,6-dioxohexahydropyrimidine-4-carboxylic acid
L-Leucine, N-[N-[N-[N-[N-[(1,1-dimethylethoxy)carbonyl]-L-tyrosyl]-O-(1,1-dimethylethyl)-D-seryl]glycyl]-L-phenylalanyl]- (9CI)
PAM BOC-L-THREONINE (BZL)
京尼平甙酸
CUPRESSUFLAVONE WITH HPLC
3-(4-FLUOROPHENYL)PROPRIONIC ACID
AMINO-(3-CHLORO-4-METHOXY-PHENYL)-ACETIC ACID
3-氨基-5-羟基吡啶二盐酸盐