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CDK4 inhibitor CDK4/Cyclin D1 inhibitor

Catalog No.B1233
Size Price Stock
10mg
$361.00
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25mg
$523.00
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50mg
$855.00
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100mg
$1,330.00
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CDK4 inhibitor

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Chemical Properties

Cas No. 1256963-02-6 SDF Download SDF
Synonyms N/A
Chemical Name 4-(3-chloro-5-propan-2-yl-1H-pyrazol-4-yl)-N-[5-[4-(dimethylamino)piperidin-1-yl]pyridin-2-yl]pyrimidin-2-amine
Canonical SMILES CC(C)C1=C(C(=NN1)Cl)C2=NC(=NC=C2)NC3=NC=C(C=C3)N4CCC(CC4)N(C)C
Formula C22H29ClN8 M.Wt 440.97
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

CDK4 inhibitor is a selective inhibitor of cyclin-dependent kinase 4 with IC50 value of 10 nM [1].

Cyclin-dependent kinase 4 (CDK4) is a Ser/Thr protein kinase and is a member of the cyclin-dependent kinase family. CDK4 plays an important role in the G1-S phase.

CDK4 inhibitor is a selective cyclin-dependent kinase 4 inhibitor. CDK4 inhibitor inhibited CDK4/Cyclin D1, CDK1/Cyclin B and CDK2/Cyclin A with IC50 values of 10 nM, 15 μM and 5.265 μM, respectively. Also, it inhibited protein kinase A (PKA) and glycogen synthase kinase (GSK3β) with IC50 values of 6.8 and 9.6 μM, respectively. In a mantle-cell lymphoma cell line Jeko-1, CDK4 inhibitor inhibited the phosphorylation level of pRb at the Ser780 site with IC50 value of 0.324 μM. Also, CDK4 inhibitor (0.37 μM) showed G1 block on cells [1].

Reference:
[1].  Cho YS, Borland M, Brain C, et al. 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. J Med Chem, 2010, 53(22): 7938-7957.