Product Name :
JAK2-IN-7
Description:
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
CAS:
Molecular Weight:
459.59
Formula:
C26H33N7O
Chemical Name:
(2E)-4-(dimethylamino)-1-[6-(5-methyl-4-[1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-ylamino)-1,2,3,4-tetrahydroisoquinolin-2-yl]but-2-en-1-one
Smiles :
CN(C)C/C=C/C(=O)N1CC2=CC=C(C=C2CC1)NC1N=CC(C)=C(N=1)C1C=NN(C=1)C(C)C
InChiKey:
SURRDPSGERGIIM-VOTSOKGWSA-N
InChi :
InChI=1S/C26H33N7O/c1-18(2)33-17-22(15-28-33)25-19(3)14-27-26(30-25)29-23-9-8-21-16-32(12-10-20(21)13-23)24(34)7-6-11-31(4)5/h6-9,13-15,17-18H,10-12,16H2,1-5H3,(H,27,29,30)/b7-6+
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively.Sunitinib medchemexpress JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3.Ascorbyl palmitate Epigenetic Reader Domain JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.|Product information|Molecular Weight: 459.59|Formula: C26H33N7O|Chemical Name: (2E)-4-(dimethylamino)-1-[6-(5-methyl-4-[1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-ylamino)-1,2,3,4-tetrahydroisoquinolin-2-yl]but-2-en-1-one|Smiles: CN(C)C/C=C/C(=O)N1CC2=CC=C(C=C2CC1)NC1N=CC(C)=C(N=1)C1C=NN(C=1)C(C)C|InChiKey: SURRDPSGERGIIM-VOTSOKGWSA-N|InChi: InChI=1S/C26H33N7O/c1-18(2)33-17-22(15-28-33)25-19(3)14-27-26(30-25)29-23-9-8-21-16-32(12-10-20(21)13-23)24(34)7-6-11-31(4)5/h6-9,13-15,17-18H,10-12,16H2,1-5H3,(H,27,29,30)/b7-6+|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (543.PMID:32202176 96 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells. JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase. JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells.|In Vivo:|JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model. JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib.|Products are for research use only. Not for human use.|