THZ2CDK7 inhibitor CAS# 1604810-84-5 |
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Quality Control & MSDS
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| Cas No. | 1604810-84-5 | SDF | Download SDF |
| PubChem ID | 78357763 | Appearance | Powder |
| Formula | C31H28ClN7O2 | M.Wt | 566.05 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 39 mg/mL (68.90 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzamide | ||
| SMILES | CN(C)CC=CC(=O)NC1=CC=CC(=C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl | ||
| Standard InChIKey | FONRCZUZCHXWBD-VGOFMYFVSA-N | ||
| Standard InChI | InChI=1S/C31H28ClN7O2/c1-39(2)15-7-14-28(40)35-21-9-5-8-20(16-21)30(41)36-22-10-6-11-23(17-22)37-31-34-19-26(32)29(38-31)25-18-33-27-13-4-3-12-24(25)27/h3-14,16-19,33H,15H2,1-2H3,(H,35,40)(H,36,41)(H,34,37,38)/b14-7+ | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.In Vitro:THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells[1].In Vivo:THZ2 (10 mg/Kg) markedly reduces the growth rate of tumors in mice and demonstrates an anti-tumor activity. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis, as indicated by immunostaining against Ki67 and cleaved Caspase 3 respectively. THZ2 in NOD-SCID mice leads to reduced body weight, suggesting that THZ2 mayt be less well-tolerated in this particular mouse strain[1]. References: | |||||
THZ2 Dilution Calculator
THZ2 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.7666 mL | 8.8331 mL | 17.6663 mL | 35.3326 mL | 44.1657 mL |
| 5 mM | 0.3533 mL | 1.7666 mL | 3.5333 mL | 7.0665 mL | 8.8331 mL |
| 10 mM | 0.1767 mL | 0.8833 mL | 1.7666 mL | 3.5333 mL | 4.4166 mL |
| 50 mM | 0.0353 mL | 0.1767 mL | 0.3533 mL | 0.7067 mL | 0.8833 mL |
| 100 mM | 0.0177 mL | 0.0883 mL | 0.1767 mL | 0.3533 mL | 0.4417 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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THZ2 is a potent and selective CDK7 inhibitor (IC50=13.9 nM).
Cyclin-dependent kinase (CDK) is a group of serine/threonine kinases. It is activated by binding to cyclin and participates in the regulation of cell cycle.
THZ2 selectively targets CDK7 and potently blocks the proliferation of triple-negative breast cancer (TNBC) cells and induces apoptotic cell death without causing alteration in cell cycle. The low nanomolar dose of THZ2 also inhibits the clonogenic growth of TNBC cells with IC50 of 10 nM.
THZ2 is well tolerant in mice as 10 mg/kg intraperitoneal treatment of THZ2 twice daily does not cause weight loss or behavioral changes. THZ2 treatment also significantly reduces the tumor growth rate mice. In addition, both acute (50 hr) or chronic (25 days) exposure to THZ markedly decreases CTD phosphorylation of RNAPII at all three phosphorylation sites as indication of CDk7 being efficiently targeted.
Reference:
1. Wang Y, Zhang T, Kwiatkowski N et al. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015 Sep 24;163(1):174-86.
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Cyclin-dependent kinase 7 inhibitor THZ2 inhibits the growth of human gastric cancer in vitro and in vivo.[Pubmed:30662617]
Am J Transl Res. 2018 Nov 15;10(11):3664-3676. eCollection 2018.
Cyclin-dependent kinase 7 (CDK7) is a member of the CDK family, which forms the CDK activating kinase complex with Cyclin H and RING finger protein Mat1 to control cell cycle progression and transcription by phosphorylating other CDKs and RNA polymerase II. In this study, we analyzed TCGA data and found that upregulation of CDK7 frequently occurred in human gastric cancer. A potent and selective irreversible CDK7 inhibitor THZ2 was able to induce cell growth inhibition, cell cycle arrest at G2/M phase and apoptosis with the increasing intracellular reactive oxidative species (ROS) levels in gastric cancer cells. Pretreatment with ROS scavenger N-acety-L-cysteine partially reversed cell apoptosis induced by THZ2. In the nude mice, THZ2 also suppressed the growth of xenograft tumors of gastric cancer. Overall, our data showed that inhibition of CDK7 with THZ2 in gastric cancer presented outstanding anticancer effect in vitro and in vivo, suggesting that CDK7 is a potential therapeutic target for gastric cancer patients.
