Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Description
ProductName AP26113 Cat No CEI-0851 Description AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 1/2. CAS No 1197958-12-5 Molecular Weight 529.01 Storage 2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO. Targets ALK, FER, ROS/ROS1, FLT3, FES/FPS IC50 0.62 nM; 1.3 nM; 1.9 nM; 2.1 nM; 3.4 nM Molecular Formula C26H34ClN6O2P Chemical Name 2,4-Pyrimidinediamine, 5-chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]- Solubility DMSO 45 mg/mL; Water <1 mg/mL; Ethanol 106 mg/mL In vitro AP26113 is highly active against both sensitive and resistant H3122 cells, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis in a dose dependent manner. AP26113 decreases p-ALK in the H3122 and H3122 CR cells, with IC50 values of 7.4 versus 16.8 nM, respectively. AP26113 decreases cell number in Ba/F3 cells expressing either native or mutant EML4-ALK with IC50 of 10 nM and 24 nM, respectively. AP26113 inhibits cell growth of SU-DHL-1, H3122 and Ba/F3-EML4-ALK v1 cell lines with GI50 of 9 nM, 4 nM and 13 nM, respectively. AP26113 inhibits phosphorylation of ALK with IC50 of 3.2 nM, 1.5 nM and 2.1 nM in Karpas-299, SU-DHL-1 and L-82 cell lines. AP26113 dose-dependently inhibits phosphorylation of ALK and ERK in Karpas-299 and H3122 cells.AP26113 inhibits cell growth with IC50 of 11 nM and 16 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK G1269S mutants). AP26113 inhibits ALK phosphorylationh with IC50 of 74 nM and 335 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK E1210K mutants). AP26113 (10 mg/kg-75 mg/kg) is efficacious in PF-02341066-resistant EML4-ALK mutant mouse xenograft models. AP26113 induces regression of tumors expressing native EML4-ALK and the G1269S and L1196M mutants at 25 mg/kg, 50 mg/kg and 50 mg/kg, respectively.AP26113 inhibits EGFR phosphorylation and viability with IC50 of 75 nM and 114 nM, respectively, in Ba/F3 cells expressing EGFR-DEL. AP26113 inhibits EGFR phosphorylation and viability with IC50s of 15 and 281 nM, respectively, in Ba/F3 cells expressing EGFR-DEL/T790M. AP26113 inhibits EGFR phosphorylation with an IC50 of 62 nM and cell growth with a GI50 of 165 nM in a NSCLC line expressing EGFR-DEL (HCC827). AP26113 inhibits EGFR phosphorylation with an IC50 of 59 nM and cell growth with a GI50 of 245 nM in HCC827 cells expressing EGFR-DEL/T790M. AP26113 potently inhibits SLC34A2-ROS-driven signaling and proliferation in a dose dependent manner in HCC78 NSCLC cells. In vivo AP26113 (< 50 mg/kg) dose-dependently inhibits p-ALK in tumor of Karpas-299 xenograft mice model. AP26113 (< 50 mg/kg) dose-dependently inhibits tumor growth in Karpas-299 xenograft mice model and H3122 xenograft mice model. AP26113 demonstrates favorable properties including moderate in vitro plasma protein binding (47%, 70% and 76% in human, rat, mouse), negligible inhibition of major CYP isoforms. AP26113 (10 mg/kg) is well-tolerated with Cmax of 2587 ng/mL and AUC of 41120 hr.ng/mL in rats.AP26113 (25 mg/kg) leads to tumor regression in HCC827(EGFR-DEL) or HCC827(EGFR-DEL/T790M) xenograft mice model. category Bulk Drug Intermediates(c1112) cas_num 1197958-12-5 Basic Info-
Product Name:
5-Chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]-2,4-pyrimidinediamine
Other Name:2,4-Pyrimidinediamine,5-chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]-;5-Chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]-2,4-pyrimidinediamine
CAS No.:1197958-12-5
Molecular Formula:C26H34ClN6O2P
InChIKeys:InChIKey=OVDSPTSBIQCAIN-UHFFFAOYSA-N
Molecular Weight:575.039301
Exact Mass:529.01
UNII:3DGD69C6PV
DSSTox ID:DTXSID30725416
Categories:
Characteristics-
PSA:
82.6
XLogP3:4.8
Density:1.29±0.1 g/cm3(Predicted)
Boiling Point:737.6±70.0 °C(Predicted)
Flash Point:399.9±35.7 °C
Refractive Index:1.626
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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Country Product Purchase Quantity Date Posted Post an enquiry for this product