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SB1317

规格或纯度: ≥98%

CAS编号: 937270-47-8
分子式: C₂₃H₂₄N₄O
分子量: 372.46
PubChem编号: 16739650

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货号 (SKU)	包装规格	是否现货	价格	数量
S127924-5mg	5mg	现货
S127924-10mg	10mg	现货
S127924-25mg	25mg	现货
S127924-50mg	50mg	现货
S127924-100mg	100mg	现货

查看相关系列

colony stimulating factor 1 receptor Inhibitor cyclin dependent kinase 1 Inhibitor cyclin dependent kinase 2 Inhibitor cyclin dependent kinase 3 Inhibitor cyclin dependent kinase 5 Inhibitor cyclin dependent kinase 9 Inhibitor fms related receptor tyrosine kinase 3 Inhibitor Janus kinase 1 Inhibitor Janus kinase 2 Inhibitor tyrosine kinase 2 Inhibitor

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基本描述

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%.

名称和标识符

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
PubChem CID	16739650
分子量	372.46

数据库链接

PubChem CID	16739650
ChEMBL Ligand	CHEMBL1944698
BindingDB Ligand	50363196
CAS Registry No.	937270-47-8

化学和物理性质

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

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JAK-STAT 细胞信号通路

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治疗肿瘤白血病 JAK家族激酶

JAK-STAT Cell Signaling Pathway

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treat tumors leukemia JAK family kinases

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参考文献

1. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M et al.. (2012) Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.. J Med Chem, 55 (1): (169-96). [PMID:22148278]
2. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.. Leukemia, 26 (2): (236-43). [PMID:21860433]
3. Poulsen A, William A, Blanchard S, Nagaraj H, Williams M, Wang H, Lee A, Sun E, Teo EL, Tan E et al.. (2013) Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).. J Mol Model, 19 (1): (119-30). [PMID:22820730]
4. Pallis M, Abdul-Aziz A, Burrows F, Seedhouse C, Grundy M, Russell N. (2012) The multi-kinase inhibitor TG02 overcomes signalling activation by survival factors to deplete MCL1 and XIAP and induce cell death in primary acute myeloid leukaemia cells.. Br J Haematol, 159 (2): (191-203). [PMID:22934750]
5. Pallis M, Burrows F, Whittall A, Boddy N, Seedhouse C, Russell N. (2013) Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells.. BMC Pharmacol Toxicol, 14 (13): (32). [PMID:23767415]

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