SML2672

Tandutinib hydrochloride

≥98% (HPLC)

• 別名: 4-[6-Methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinyl]-N-[4-(1-methylethoxy)phenyl]-1-piperazinecarboxamide hydrochloride, CT 53518 hydrochloride, CT-53518 hydrochloride, CT53518 hydrochloride, MLN 518 hydrochloride, MLN-518 hydrochloride, MLN518 hydrochloride, N-(4-Isopropoxyphenyl)-4-(6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-yl)piperazine-1-carboxamide hydrochloride
• 実験式（ヒル表記法）: C₃₁H₄₂N₆O₄ · xHCl
• CAS番号: 387867-13-2
• 分子量: 562.70 (free base basis)
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 保管条件: desiccated
• 色: white to beige
• 溶解性: H₂O: 2 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: N5(CCCCC5)CCCOc1cc2ncnc(c2cc1OC)N3CCN(CC3)C(=O)Nc4ccc(cc4)OC(C)C
• InChI: 1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)
• InChI Key: UXXQOJXBIDBUAC-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

Orally active, potent βPDGFR, c-Kit, Flt3 (Flk2, Stk1) receptor tyrosine kinase inhibitor with anti-leukemia efficacy in vitro and in vivo.

Tandutinib (CT53518, MLN518) is a potent receptor tyrosine kinase inhibitor against PDGFRβ, c-Kit, Flt3 (IC50 = 0.20, 0.17, 0.22, 3.43 μM, respectively, against 8 nM PDGF-BB induced autophosphorylation of βPDGFR, βPDGFR/c-Kit, βPDGFR/Flt3, βPDGFR/CSF-1R chimera expressed in CHO cells; IC50 =30 μM against KDR, EFGR, FGFR, InsR, Abl, Src, PKA, PKC, ERK2, MEK1, MKK4/6, p38). Tandutinib prolongs the survival in murine CMML (Baf3 with Tel/βPDGFR chimera) and Flt-3/ITD AML leukemia models (60 mg/kg bid p.o.) with good oral bioavailability.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable