产品名称

英文名称：SB1317

同义词

SB1317、Zotiraciclib、1204918-72-8、TG-02、937270-47-8、SB-1317、TG02、SB-1317 free base、Zotiraciclib [USAN]、Ex 45、EX45、CHEMBL1944698、(E/Z)-Zotiraciclib、40D08182TT、TG02 (SB1317)、Zotiraciclib (USAN)、TG02 (Double bond E)、(E)-6-methyl-12-oxa-3,6-diaza-2(4,2)-pyrimi

产品性质

CAS编号：937270-47-8

分子式：C23H24N4O

分子量：372.46

PubChem编号：16739650

英文别名：SB1317|Zotiraciclib|1204918-72-8|TG-02|937270-47-8|SB-1317|TG02|SB-1317 free base|Zotiraciclib [USAN]|Ex 45|EX45|CHEMBL1944698|(E/Z)-Zotiraciclib|40D08182TT|TG02 (SB1317)|Zotiraciclib (USAN)|TG02 (Double bond E)|(E)-6-methyl-12-oxa-3,6-diaza-2(4,2)-pyrimi

规格或纯度：≥98%

英文名称：SB1317

生化机理：TG02 is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. TG02 is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis. In vivo, TG02 exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling. TG02 induces tumor regression after oral dosing on both daily and intermittent schedules in a murine model of mutant-FLT3 leukemia (MV4-11) and prolongs survival in a disseminated AML model with wild-type FLT3 and JAK2 (HL-60). TG02 is active in various models of leukemia and provide a rationale for the ongoing clinical evaluation of TG02 in patients with advanced leukemias.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍 SB1317是一种强效的细胞周期蛋白依赖性激酶(CDKs)\FMS样酪氨酸激酶3(FLT3)及Janus激酶2(JAK2)抑制剂,对CDK2\JAK2及FLT3的IC50值分别为13 nM\56 nM及73 nM.CDKs是调节细胞周期的丝氨酸苏氨酸激酶.JAK2是一种不可逆的细胞内酪氨酸激酶,其经由JAK-STAT信号通路转导细胞因子介导的信号.FLT3是一种细胞因子受体,在造血干细胞的正常发展中发挥着重要作用.在表达荧光素酶的MM1S细胞中,SB1317克服了IL-6赋予的增殖/保护优势.在MM1S细胞中,SB1317增加G2 / M期的细胞比例,且减少S期的细胞.另外,SB1317增加亚G0区的细胞数.在人多发性骨髓瘤浆细胞瘤异种移植CB17-SCID小鼠模型(硼替佐米敏感性MM1S模型和更具硼替佐米耐药性的OPM2模型)中,SB1317显著抑制肿瘤生长.在皮下AML模型中,连续21天每天给小鼠分别服用10\20或40 mg/kg剂量的SB1317可使平均肿瘤体积分别减小53%\61%及113%.

ALogP：4.2

IUPAC Name：(16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene

INCHI：InChI=1S/C23H24N4O/c1-27-13-3-2-4-14-28-21-10-6-8-19(16-21)22-11-12-24-23(26-22)25-20-9-5-7-18(15-20)17-27/h2-3,5-12,15-16H,4,13-14,17H2,1H3,(H,24,25,26)/b3-2+

InChi Key：VXBAJLGYBMTJCY-NSCUHMNNSA-N

Canonical SMILES：CN1CC=CCCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1

Isomeric SMILES：CN1C/C=C/CCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1

PubChem CID：16739650

ChEMBL Ligand：CHEMBL1944698

BindingDB Ligand：50363196

CAS Registry No.：937270-47-8

溶解性：insoluble in H2O; ≥44.87 mg/mL in DMSO; ≥3.98 mg/mL in EtOH with gentle warming and ultrasonic

产品包装