AZD-5991
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $2025 | To Be Confirmed |
| 200mg | $3035 | To Be Confirmed |
| 500mg | $5125 | To Be Confirmed |
: Cat #: V4341 CAS #: 2143061-81-6 Purity ≥ 98%
Description: AZD-5991 (AZD5991) is a novel, potent, rationally designed macrocyclic molecule and selective MCL-1 inhibitor with anticancer activity.
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| Molecular Weight (MW) | 672.26 |
|---|---|
| Molecular Formula | C35H34ClN5O3S2 |
| CAS No. | 2143061-81-6 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | CN1C(C(O)=O)=C(CCCOC2=C(C=CC=C3)C3=CC(SC4)=C2)C5=CC=C(Cl)C(C6=C(C)N(C)N=C6CSCC7=NN(C)C4=C7)=C51 |
| Synonyms | AZD5991; AZD-5991; AZD 5991; |
| Protocol | In Vitro | The selectivity of AZD-5991 is evaluated against pro-survival Bcl-2 family members using FRET assays. AZD-5991 is selective for Mcl-1 (IC50 0.72 nM, Ki=200 pM) vs. Bcl-2 (IC50=20 µM, Ki=6.8 µM), Bcl-xL (IC50=36 µM, Ki=18 µM), Bcl-w (IC50=49 µM, Ki=25 µM), and Bfl-1 (IC50=24 µM, Ki=12 µM). MOLP-8, MV4-11, and NCI-H23 cells are treated with AZD5991 (EC50=0.033, 0.024, 0.19 µM, respectively).AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia, by activating the Bak-dependent mitochondrial apoptotic pathway. AZD5991 reduces the levels of Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines further supporting the notion that activation of caspases by AZD5991 reduces Mcl-1 protein levels in AZD5991-sensitive cell lines. |
|---|---|---|
| In Vivo | A single intravenous (i.v.) dose of AZD5991 leads to a dose-dependent antitumor effect ranging from tumor growth inhibition (TGI) to tumor regression (TR). Ten days after treatment, AZD5991 shows 52% and 93% TGI (p<0.0001) at 10 and 30 mg/kg, respectively. At the same time point, AZD5991 at 60 mg/kg leads to 99% TR with no detectable tumors in 6 out of 7 mice, while complete TR is seen in 7 out of 7 mice in the 100 mg/kg dose group. AZD5991 also shows a dose-dependent duration of response with tumors in the 100 mg/kg group growing back later than those in the 60 mg/kg group. The magnitude of in vivo tumor efficacy is correlated with activation of caspase-3 in the tumor and concentration of AZD5991 in plasma. Treatment with AZD5991 was well tolerated at all dose levels with no significant body weight loss. A single dose of AZD5991 36 days after the first dose causes tumor regression in 4 out of 4 mice. In mice dosed with AZD5991 at 100 mg/kg on day 0 and day 1, tumors grow back later than those dosed with a single dose of AZD5991 at the same dose level. |
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 | 1.4875 mL | 7.4376 mL | 14.8752 mL | 29.7504 mL |
| 5mM | 0.2975 mL | 1.4875 mL | 2.9750 mL | 5.9501 mL |
| 10mM | 0.1488 mL | 0.7438 mL | 1.4875 mL | 2.9750 mL |
| 20mM | 0.0744 mL | 0.3719 mL | 0.7438 mL | 1.4875 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
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%Tween 80
+
%ddH2O
Calculation Results:
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Method for preparing DMSO master liquid:
mg
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,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.