CNX-1351
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
100mg | $745 | Check With Us |
250mg | $1450 | Check With Us |
500mg | $2175 | Check With Us |
Cat #: V18587 CAS #: 1276105-89-5 Purity ≥ 99%
Description: CNX-1351 (CNX1351; CNX 1351) is a novel, potent, covalent and selective inhibitor of PI3Kα with anticancer activity.
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Molecular Weight (MW) | 573.71 |
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Molecular Formula | C30H35N7O3S |
CAS No. | 1276105-89-5 |
SMILES Code | C/C(C)=C/C(CCC(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)=O)=O |
Synonyms | CNX1351; CNX 1351; CNX-135 |
Protocol | In Vitro | CNX-1351 is able to potently (EC50<100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI50<100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC50 of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with different PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. Both PIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI50 of 78 and 55 nM, respectively). |
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In Vivo | CNX-1351 inhibits p-AktSer473 in mouse spleens and bonds to PI3Kα in vivo. CNX-1351 is delivered into the intraperitoneal cavity of nude mice at 100 mg/kg once a day for 5 consecutive days (n=3 mice per group). Spleens are harvested from the mice at the indicated times after the last dose (1-24 h) and interrogated by immunoblot for P-AktSer473 or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-AktSer473 at 1 and 4 h after last dose. |
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 | 1.7430 mL | 8.7152 mL | 17.4304 mL | 34.8608 mL |
5mM | 0.3486 mL | 1.7430 mL | 3.4861 mL | 6.9722 mL |
10mM | 0.1743 mL | 0.8715 mL | 1.7430 mL | 3.4861 mL |
20mM | 0.0872 mL | 0.4358 mL | 0.8715 mL | 1.7430 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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