387867-13-2 Usage
Description
Tandutinib, an N-arylpiperazine derivative, is a potent antagonist of platelet-derived growth factor receptor β (PDGFRβ), FLT3, and c-Kit, with IC50 values of 200, 220, and 170 nM, respectively. It is a white solid that also less potently inhibits macrophage colony-stimulating factor 1 receptor (IC50 = 3.4 μM) and does not significantly inhibit other tyrosine or serine/threonine kinases. Tandutinib is used as an oral, small-molecule inhibitor for the treatment of various cancer indications, including acute myelogenous leukemia (AML) and myelodysplastic syndrome.
Uses
Used in Oncology:
Tandutinib is used as an anticancer agent for the treatment of AML and other cancer indications. It acts as an oral, small-molecule inhibitor of FLT3, blocking the growth of cells expressing an internal tandem duplication within the juxtamembrane domain of the FLT3 receptor, which is found in some AML cells. Tandutinib also impairs the growth of colon cancer cells through its actions on the c-Kit receptor and reverses multidrug resistance in vitro by impairing the efflux activity of the multidrug resistance protein 7.
Used in Antipsoratic Applications:
Tandutinib is used as an antipsoratic agent, helping to manage and treat psoriasis, a chronic skin condition characterized by the rapid growth and shedding of skin cells.
Used in Combination Therapy for AML:
In a phase I/II clinical trial, Tandutinib displayed promising antileukemic activity (90% complete remissions) when administered in combination with cytarabine and daunorubicin for the treatment of newly diagnosed AML patients. This combination therapy enhances the efficacy of Tandutinib and improves treatment outcomes for patients with AML.
references
[1] kelly lm1, yu jc, boulton cl, apatira m, li j, sullivan cm, williams i, amaral sm, curley dp, duclos n, neuberg d, scarborough rm, pandey a, hollenbach s, abe k, lokker na, gilliland dg, giese na. ct53518, a novel selective flt3 antagonist for the treatment of acute myelogenous leukemia (aml). cancer cell. 2002 jun;1(5):421-32.
Check Digit Verification of cas no
The CAS Registry Mumber 387867-13-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,8,7,8,6 and 7 respectively; the second part has 2 digits, 1 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 387867-13:
(8*3)+(7*8)+(6*7)+(5*8)+(4*6)+(3*7)+(2*1)+(1*3)=212
212 % 10 = 2
So 387867-13-2 is a valid CAS Registry Number.
InChI:InChI=1/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)
387867-13-2Relevant articles and documents
LACTATE SALT OF 4-[6-METHOXY-7-(3-PIPERIDIN-1-YL-PROPOXY)QUINAZOLIN-4-YL]PIPERAZINE-1-CARBOXYLIC ACID(4-ISOPROPOXYPHENYL)-AMIDE AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF CANCER AND OTHER DISEASES OR DISORDERS
-
, (2015/05/26)
This invention provides a compound of formula (I): or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; processes for the synthesis or manufacture of the compound of formula (I), or a cryst
Improved synthesis of substituted 6,7-dihydroxy-4-quinazolineamines: Tandutinib, erlotinib and gefitinib
Knesl, Petr,Roeseling, Dirk,Jordis, Ulrich
, p. 286 - 297 (2007/10/03)
The synthesis of three substituted 6,7-dihydroxy-4-quinazolineamines: tandutinib (1), erlotinib (2) and gefitinib (3) in improved yields is reported. The intermediates were characterized by NMR and the purities determined by HPLC.
