THZ1
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $750 | Check With Us |
500mg | $1250 | Check With Us |
1g | $1875 | Check With Us |
Cat #: V2557 CAS #: 1604810-83-4 Purity ≥ 98%
Description: THZ1 (THZ-1) is a novel, potent, selective and covalent/irreversible CDK7 inhibitor (IC50 = 3.2 nM) with anticancer activity.
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- Physicochemical and Storage Information
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- Related Biological Data
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Molecular Weight (MW) | 566.05 |
---|---|
Molecular Formula | C31H28ClN7O2 |
CAS No. | 1604810-83-4 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 28.3mg/mLr |
Water: <1 mg/mLr | |
Ethanol: N/A | |
Synonyms | THZ-1; THZ 1; THZ1 |
Protocol | In Vitro | THZ1 inhibits Jurkat cell and Loucy cell with IC50 of 50 nM, and 0.55 nM, respectively. THZ1 (9, 27, 83, 250, 750, and 2500 nM) inhibits CDK12 but at higher concentrations compared to CDK7. THZ1 (1 μM) irreversibly inhibits RNAPII CTD and CAK phosphorylation. THZ1 (2.5 µM) irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7 in Hela S3 cells. THZ1 (250 nM) causes decreased cellular proliferation and an increase in apoptotic index with concomitant reduction in anti-apoptotic proteins, most notably MCL-1 and XIAP in T-ALL cell lines |
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In Vivo | THZ1 (10 mg/kg) demonstrates potent killing of primary chronic lymphocytic leukemia (CLL) cells and anti-proliferative activity against primary TALL cells and in vivo against a human T-ALL xenograft |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7666 mL | 8.8331 mL | 17.6663 mL | 35.3326 mL |
5mM | 0.3533 mL | 1.7666 mL | 3.5333 mL | 7.0665 mL |
10mM | 0.1767 mL | 0.8833 mL | 1.7666 mL | 3.5333 mL |
20mM | 0.0883 mL | 0.4417 mL | 0.8833 mL | 1.7666 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.