PKI402(PKI-402)|pan PI3K/mTOR inhibitor|DC Chemicals

Cas No.:	1173204-81-3
Chemical Name:	1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(1-methylpiperazine-4-carbonyl)phenyl)urea
Synonyms:	PKI 402; PKI402;PKI-402
SMILES:	CCN1N=NC2=C1N=C(N=C2N3CCOCC3)C4=CC=C(C=C4)NC(NC5=CC=C(C=C5)C(N6CCN(CC6)C)=O)=O
Formula:	C₂₉H₃₄N₁₀O₃
M.Wt:	570.65
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Equivalent to the IC50 For wild-type PI3Kα, PKI-402 inhibits E545K and H1047R PI3Kα mutants with IC50 of 3 nM. In a panel of 236 human protein kinases, PKI-402 only displays inhibitory activity against C-Raf and B-Raf with IC50 of 7 μM, and displays little activity against all other kinases with IC50 of > 10 μM. PKI-402 inhibits the growth of human tumor cell lines with IC50 of 6-349 nM. Consistently, PKI-402 inhibits phosphorylation of PI3K and mTOR effector proteins, particularly phosphorylated Akt (p-Akt) at T308 and S473 with IC50 of <10 nM and <30 nM, respectively. PKI-402 inhibits both p70S6K and 4EBP1 phosphorylation with IC50 of <10 nM. PKI-402 inhibits Akt phosphorylation of PRAS40 at T246 with IC50 of <30 nM, and inhibits Akt phosphorylation of ENOS at S1177 and GSK3α/GSK3β at S9/S21 with IC50 of <10 nM. In MDAMB-361, a breast tumor line with mutant PI3K-α (E545K) and elevated levels of Her2 receptor, PKI-402 treatment induces cleaved poly(ADP-ribose) polymerase (PARP), a marker For apoptosis. Less than 10% of MDAMB-361 cells exposed to PKI-402 at 0.3 μM (or higher) For 24 hours remain viable. Single dose of PKI-402 (100 mg/kg) suppresses Akt phosphorylation (at T308) and induces cleaved PARP in MDA-MB-361 tumors. In normal tissue (heart and lung), PKI-402 (100 mg/kg) has minimal effect on p-Akt, with no detectable cleaved PARP. Consistently, PKI-402 at 100 mg/kg (daily For 5 days, one round) reduces initial tumor volume of 260 mm3 to 129 mm3 and prevents tumor regrowth For 70 days in MDA-MB-361. PKI-402 significantly inhibits the growth of A549 tumors in nude mice at 25 mg/kg and 50 mg/kg. PKI-402 at 100 mg/kg (daily For 5 days, one round) causes significant (P < 0.01) reduction in tumor growth of U87MG.For the detailed information of PKI402, the solubility of PKI402 in water, the solubility of PKI402 in DMSO, the solubility of PKI402 in PBS buffer, the animal experiment (test) of PKI402, the cell expriment (test) of PKI402, the in vivo, in vitro and clinical trial test of PKI402, the EC50, IC50,and Affinity of PKI402, Please contact DC Chemicals.

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