5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine
CAS: 944396-07-0;1202777-78-3
Molecular Formula: C18H21F3N6O2
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine - Names and Identifiers
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine - Physico-chemical Properties
| Molecular Formula | C18H21F3N6O2 |
| Molar Mass | 410.39 |
| Density | 1.382 |
| Melting Point | 143-147°C |
| Boling Point | 645.7±65.0 °C(Predicted) |
| Solubility | DMSO 82 mg/mL Water <1 mg/mL Ethanol 2 mg/mL |
| Appearance | White powder. |
| Color | White |
| pKa | 5.94±0.50(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Use | A PI 3-kinase family inhibitor |
| In vitro study | BKM120 has anti-proliferative activity when acting on cell lines deregulated by PI3K, including A2780, U87MG, MCF7 and DU145, with a GI50 of 0.1-0.7 nM. BKM120 induces apoptosis of multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266), resulting in an increase in G1 phase cells and a decrease in S phase cells. BKM120 induces apoptosis in CD138 primary MM cells and is less toxic when acting on CD138 − stromal cells. BKM120 can cause up-regulation of BimS and down-regulation of XIAP. BKM120 acts on human gastric cancer cell lines, reduces mTOR downstream signaling, and has anti-proliferative activity. BKM120 can be enhanced by p-ERK or p-STAT3 in the KRAS mutant gastric cancer cell line. BKM120 in combination with a STAT3 blocker induces apoptosis in cells containing mutated KRAS, with a synergistic effect, but not in KRAS wild-type cells. BKM120 regulates mitotic collapse primarily through Aurora B kinase. BKM120 has anti-proliferative activity when acting on cell lines deregulated by PI3K, including A2780, U87MG, MCF7 and DU145, with a GI50 of 0.1-0.7 nM. BKM120 induces apoptosis of multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266), resulting in an increase in G1 phase cells and a decrease in S phase cells. BKM120 induces apoptosis in CD138 primary MM cells and is less toxic when acting on CD138 − stromal cells. BKM120 can cause up-regulation of BimS and down-regulation of XIAP. BKM120 acts on human gastric cancer cell lines, reduces mTOR downstream signaling, and has anti-proliferative activity. BKM120 can be enhanced by p-ERK or p-STAT3 in the KRAS mutant gastric cancer cell line. BKM120 in combination with a STAT3 blocker induces apoptosis in cells containing mutated KRAS, with a synergistic effect, but not in KRAS wild-type cells. BKM120 regulates mitotic collapse primarily through Aurora B kinase. |
| In vivo study | BKM120 completely inhibited pAKTser473 at a dose of 30, 60, or 100 mg/kg for A2780 xenografts. BKM120 showed anticancer activity in the U87MG glioma model at doses of 30 and 60 mg/kg. Treatment of BKM120 daily at a dose of 5 μm/kg in a durable ARP1 SCID murine model resulted in a significant reduction in tumor volume and K-chain levels. at a dose of 30, 60, or 100 mg/kg, BKM120 completely inhibited pAKTser473 in A2780 xenograft. BKM120 showed anticancer activity in the U87MG glioma model at doses of 30 and 60 mg/kg. Treatment of BKM120 daily at a dose of 5 μm/kg in a durable ARP1 SCID murine model resulted in a significant reduction in tumor volume and K-chain levels. |
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine - Risk and Safety
| HS Code | 29349990 |
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine - Introduction
BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibition. When p110α/β/δ/γ is applied, IC50 is 52 nM/166 nM/116 nM/262 nM, respectively. The effect on VPS34, mTOR and DNAPK is reduced, and there is almost no inhibitory activity on PI4Kβ. Phase 2.
Last Update：2022-10-16 17:30:18
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine - Reference Information
| oral pan-PI3K inhibitor | Buparlisib(AN2025)(BKM120) is an oral pan-PI3K inhibitor with tumor immunity (I/O) effect, which has shown clinical activity in patients with solid tumors and hematological malignancies, the global phase 2 clinical trial of paclitaxel in the treatment of head and neck squamous cell carcinoma has been completed, and the drug safety is manageable. It has obtained the fast-track qualification (Fast-Track) of the US Food and Drug Administration (FDA). |
| indication | Buparlisib was developed by Novartis and was in clinical phase III, but the study has been terminated and has been used to treat locally advanced or metastatic breast cancer that is positive for postmenopausal estrogen receptor and negative for human epidermal growth factor receptor 2(HER2). At the same time, the company is also in the treatment of follicular lymphoma, gastrointestinal stromal tumors, mantle cell lymphoma, prostate cancer, diffuse large B cell lymphoma, non-small cell lung cancer, hepatocellular carcinoma, myelofibrosis, Phase II clinical study of advanced endometrial cancer, melanoma, bladder cancer, pancreatic cancer and malignant glioma. The compound is a pan-class I PI3K inhibitor that acts on p110α/β/δ/γ with IC50 of 52nM / 166nM / 116nM/262nM, respectively. |
Last Update：2024-04-09 19:05:03
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Product Name: Buparlisib Visit Supplier Webpage Request for quotationCAS: 944396-07-0
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Product Name: BKM120 Visit Supplier Webpage Request for quotationCAS: 944396-07-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Buparlisib Visit Supplier Webpage Request for quotationCAS: 944396-07-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: BKM120 Visit Supplier Webpage Request for quotationCAS: 944396-07-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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