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Product details

名称

CCT244747

分子类型

小分子

英文名称

CCT244747

货号

C648940-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC 50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC 50 of 29 nM. In Vitro CCT244747 poorly inhibits CHK2 (IC 50 >10 μM) and CDK1 (IC 50 >10 μM). CCT244747 has potent activities against CHK1, RSK1, RSK2, AMPK, BRSK1, IRAK1,and TrkA, with >80% inhibition. CCT244747 (10 μM) exhibits In Vivo CCT244747 (100 mg/kg po, qd7d) significantly reduces tumor burden in human tumor xenografts. CCT244747 (100-300 mg/kg, po) inhibits gemcitabine-induced pS296 CHK1 for up to 24 h in HT29 colon tumor xenografts . CCT244747 (75 mg/kg, p.o.) in combination with gemcitabine has potent antitumor effects in HT29 colon tumor xenografts and Calu6 human lung cancer xenografts. CCT244747 (150 mg/kg p.o.) also shows antitumor activities with irinotecan in SW620 human colon tumor xenografts. CCT244747 (100 mg/kg, p.o.) exhibits radiosensitization activity in Cal27 xenografts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Chk1 7.7 nM (IC 50 )

生化机理

CCT244747 是一种强效、可口服的高选择性 CHK1 抑制剂，其 IC 50 为 7.7 nM；CCT244747 还能减弱 G2 检查点，其 IC 50 为 29 nM。

CAS号

1404095-34-6

分子式

C20H24N8O2

分子量

408.47 g/mol

PubChem编号

54758482

Isomeric SMILES

C[C@H](CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C(C(=C2)OC)C3=CN(N=C3)C

IIUPAC Name

3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-methoxy-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]pyrazine-2-carbonitrile

INCHI

1S/C20H24N8O2/c1-13(11-27(2)3)30-20-16(7-21)22-10-19(26-20)25-18-6-17(29-5)15(9-23-18)14-8-24-28(4)12-14/h6,8-10,12-13H,11H2,1-5H3,(H,23,25,26)/t13-/m1/s1

InChi Key

IENLGMOXAQMNEH-CYBMUJFWSA-N

Smiles

CC(CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C(C(=C2)OC)C3=CN(N=C3)C

PubChem CID

54758482

溶解性

DMSO : 50 mg/mL (122.41 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

408.202 Da

单同位素质量Monoisotopic Mass

408.202 Da

拓扑极表面积Topological Polar Surface Area

114.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

584

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

1.7

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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