Product Name :
CCT244747
Description:
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
CAS:
1404095-34-6
Molecular Weight:
408.46
Formula:
C20H24N8O2
Chemical Name:
3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl]aminopyrazine-2-carbonitrile
Smiles :
CN(C)C[C@@H](C)OC1=NC(=CN=C1C#N)NC1=CC(OC)=C(C=N1)C1C=NN(C)C=1
InChiKey:
IENLGMOXAQMNEH-CYBMUJFWSA-N
InChi :
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
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:
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.|Product information|CAS Number: 1404095-34-6|Molecular Weight: 408.46|Formula: C20H24N8O2|Chemical Name: 3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl]aminopyrazine-2-carbonitrile|Smiles: CN(C)C[C@@H](C)OC1=NC(=CN=C1C#N)NC1=CC(OC)=C(C=N1)C1C=NN(C)C=1|InChiKey: IENLGMOXAQMNEH-CYBMUJFWSA-N|InChi: 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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 50 mg/mL (122.1-Bromooctane Biological Activity 41 mM; Need ultrasonic).Tween 80 medchemexpress |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.PMID:35195389 |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:|CCT244747 poorly inhibits CHK2 (IC50 >10 μM) and CDK1 (IC50 >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.|Products are for research use only. Not for human use.|