1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea
PKI-402
CAS: 1173204-81-3
Molecular Formula: C29H34N10O3
1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea - Names and Identifiers
| Name | PKI-402 |
| Synonyms | PKI402 CS-167 PKI-402 1-(4-(3-Ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiper 1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiperazine-1-carbonyl)phenyl)urea 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 1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea Urea, N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]- |
| CAS | 1173204-81-3 |
1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea - Physico-chemical Properties
| Molecular Formula | C29H34N10O3 |
| Molar Mass | 570.65 |
| Density | 1.43 |
| Boling Point | 670.6±55.0 °C(Predicted) |
| pKa | 13.80±0.70(Predicted) |
| Storage Condition | -20℃ |
| Use | PKI-402 is an effective, pan-PI3K/mTOR dual inhibitor, targeting PI3Kα/β/γ/δ and mTOR,IC50 is 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively, and also effectively acting on PI3Kα mutant E545K and H1047R. |
| In vitro study | 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. |
| In vivo study | 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. |
1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.752 ml | 8.762 ml | 17.524 ml |
| 5 mM | 0.35 ml | 1.752 ml | 3.505 ml |
| 10 mM | 0.175 ml | 0.876 ml | 1.752 ml |
| 5 mM | 0.035 ml | 0.175 ml | 0.35 ml |
Last Update：2024-01-02 23:10:35
![1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea](http://res.chembk.com/assets/str/2d/1/11/1173204-81-3.png)
Supplier List
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185
Wechat: chinaskyrun
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: PKI-402 Visit Supplier Webpage Request for quotation
CAS: 1173204-81-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1173204-81-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185
Wechat: chinaskyrun
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: PKI-402 Visit Supplier Webpage Request for quotationCAS: 1173204-81-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: PKI-402 Visit Supplier Webpage Request for quotation
CAS: 1173204-81-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1173204-81-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea
(2S,3R)-1-(tert-Butoxycarbonyl)-3-isopropylpyrrolidine-2-carboxylic acid
376612-52-1
335403-20-8
1-bromo-3-(difluoromethyl)naphthalene
1613482-34-0
3-(1,5-diethenyl-3-{[ethenyl(dimethyl)silyl]oxy}-1,1,5,5-tetramethyltrisiloxan-3-yl)propyl 2-methylprop-2-enoate
Melithiazole
113365-44-9
1-Acetyloxy-2-hydroxy-12,15-heneicosadien-4-one
(2S,3R)-1-(tert-Butoxycarbonyl)-3-isopropylpyrrolidine-2-carboxylic acid
376612-52-1
335403-20-8
1-bromo-3-(difluoromethyl)naphthalene
1613482-34-0
3-(1,5-diethenyl-3-{[ethenyl(dimethyl)silyl]oxy}-1,1,5,5-tetramethyltrisiloxan-3-yl)propyl 2-methylprop-2-enoate
Melithiazole
113365-44-9
1-Acetyloxy-2-hydroxy-12,15-heneicosadien-4-one