Identification | Back Directory | [Name]
SB1317 | [CAS]
937270-47-8 | [Synonyms]
CS-915 TG02;TG-02 (E/Z)-TG02 (E/Z)-SB1317 TG-02/SB-1317 SB1317, >=98% (E/Z)-Zotiraciclib Zotiraciclib free base Zotiraciclib (SB1317) HCl SB1317(TG-02) hydrochloride TG02; SB 1317; TG 02; SB-1317; TG-02 14-Methyl-20-oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene 20-Oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 14-methyl- multiple myeloma,JAK2,Fms like tyrosine kinase 3,Cyclin dependent kinase,JAK,FLT3,Janus kinase,CD135,leukemias,Inhibitor,CDK,CDK2,Cluster of differentiation antigen 135,inhibit,cancer,(E/Z)-Zotiraciclib,(E/Z) Zotiraciclib,(E/Z)Zotiraciclib | [Molecular Formula]
C23H24N4O | [MDL Number]
MFCD22124499 | [MOL File]
937270-47-8.mol | [Molecular Weight]
372.46 |
Chemical Properties | Back Directory | [Boiling point ]
575.5±60.0 °C(Predicted) | [density ]
1.16±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥44.87 mg/mL in DMSO; ≥3.98 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
8.03±0.20(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
TG 02 is a cyclin dependent kinase inhibitors (CDK inhibitors) for the treatment of chronic lymphocytic leukemia. | [in vivo]
(E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth[1].?
(E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners[1]. Animal Model: | Male BALB/c mice with HCT-116 colon cancer cells xenografts[1] | Dosage: | 50 and 75 mg/kg | Administration: | Oral gavage; 50 and 75 mg/kg once daily for 3 weeks | Result: | Significantly inhibited the growth of tumors with a mean TGI of 82%.
|
Animal Model: | Male BALB/c mice with lymphoma Ramos cells xenografts[1] | Dosage: | 15 and 75 mg/kg | Administration: | Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.) | Result: | Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.
|
| [IC 50]
CDK2: 13 nM (IC50); JAK2: 73 nM (IC50); FLT3: 56 nM (IC50) | [storage]
Store at -20°C |
|
|