ZINC02557947
AG-490 (Tyrphostin B42)
CAS: 133550-30-8
Molecular Formula: C17H14N2O3
ZINC02557947 - Names and Identifiers
ZINC02557947 - Physico-chemical Properties
| Molecular Formula | C17H14N2O3 |
| Molar Mass | 294.3 |
| Density | 1.337 |
| Melting Point | 215°C(lit.) |
| Boling Point | 615.2±55.0 °C(Predicted) |
| Solubility | DMSO:58 mg/mL (197.07 mM);Water Insoluble;Ethanol :6 mg/mL (20.38 mM) |
| Appearance | Yellow powder |
| Color | yellow |
| pKa | 8.75±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO, DMF, or ethanol may be stored at -20°C for up to 1 month. |
| MDL | MFCD00236452 |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vitro study | AG-490 inhibited EGF-dependent HER 14 cell proliferation with an IC50 of 3.5 μm. Consistent with JAK2, which specifically acts on pre-B-cell acute leukemia (ALL) cells to inhibit constitutive activation, 5 μm AG-490 almost completely inhibited the growth of ALL cells by inducing programmed cell death, and the normal hematopoietic function will not cause harmful effects. AG-490 does not inhibit Lck, Lyn, Btk, Syk, and Src activation. AG-490 (60-100 μm) inhibits Stat3 by inhibiting the activity of JAK3 and STAT5a/B. AG-490 potently inhibits human T cell growth regulated by IL-2 with an IC50 of 25 μm. Although 5 μm AG-490 alone had no effect on FDrv210H cell proliferation, AG-490 could synergize STI571 while potentiating STI571 inhibition p210AG-490 acts on MOPC, MPC11, and S194 cells, significantly Inhibiting Stat3 constitutive activation, leading to significant apoptosis, in a dose-dependent manner. AG-490 (100 μm) inhibited Akt phosphorylation, inhibited nuclear factor-kappa B activation, and activated GSK-3β, resulting in a c-Myc reduction. AG-490 (50 μm) induced apoptosis in BaF3 cells expressing Bcr-Abl mutant T315I and E255K anti-Imatinib. 30 μm AG-490 inhibited not only Epo-induced wild-type JAK2 phosphorylation, but also constitutive JAK2 V617F mutant phosphorylation. AG-490 effectively inhibits JAK 2 V617F in BaF3 cells Mutation-induced cytokine-independent cell growth. |
| In vivo study | AG-490 treatment significantly reduced CD45 in vivo, and AG-490 treatment caused apoptosis of mouse myeloma cells, but did not inhibit IL-12-induced macrophage activation and IFN-γ production. Consistent with the inhibition of JAK2 V617F mutation activity in vitro, AG-490 treated with 0.5 mg per day for 10 days in nude mice efficiently inhibited JAK2 V617F mutation-induced tumor formation and tumor cell invasion. |
ZINC02557947 - Risk and Safety
| Risk Codes | R36/37/38 - Irritating to eyes, respiratory system and skin. R50 - Very Toxic to aquatic organisms R25 - Toxic if swallowed |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all |
| WGK Germany | 1 |
| RTECS | UC6316197 |
| HS Code | 29269090 |
| Hazard Class | 6.1 |
| Packing Group | III |
ZINC02557947 - Introduction
AG-490 (Tyrphostin B42) is an EGFR inhibitor. In cell-free test, IC50 is 0.1 μM, which is 135 times more selective than ErbB2. It also has inhibitory effect on JAK2 and has no inhibitory activity on Lck,Lyn,Btk,Syk and Src.
Last Update：2022-10-16 17:31:08
ZINC02557947 - Reference Information
| biological activity | AG-490 (Tyrphostin B42, Zinc02557947) is an EGFR inhibitor. in cell-free test, IC50 is 0.1 μM, which is 135 times more selective than ErbB2, and also has inhibitory effect on JAK2, Lck,Lyn,Btk, syk and Src had no inhibitory activity. |
| target | TargetValue JAK2 (V617F) () EGFR (Cell-free say) 0.1 μM |
| Target | Value |
| JAK2 (V617F) () | |
| EGFR (Cell-free assay) | 0.1 μM |
| in vitro study | AG-490 inhibited EGF-dependent HER 14 cell proliferation with IC50 of 3.5 μM. Consistent with JAK2, which specifically acts on pre-B cell acute leukemia (ALL) cells to inhibit constitutive activation, 5 μM AG-490 almost completely inhibits the growth of all ALL cells by inducing programmed cell death, without causing harmful effects on normal hematopoietic function. AG-490 does not inhibit Lck, Lyn, Btk, Syk, and Src activation. AG-490 (60-100 μM) inhibits Stat3 by inhibiting JAK3 and STAT5a/B. AG-490 effectively inhibited IL-2-regulated human T cell growth with an IC50 of 25 μM. Although 5 μM AG-490 alone has no effect on FDrv210H cell proliferation, AG-490 can cooperate with STI571 to enhance STI571 inhibitory p210AG-490 on MOPC, MPC11, and S194 cells, significantly inhibiting Stat3 constitutive activation, leading to significant apoptosis, which is dose-dependent. AG-490 (100 μM) inhibits Akt phosphorylation, inhibits nuclear factor-κB activation, and activates GSK-3β, resulting in reduced c-Myc. AG-490 (50 μM) can induce apoptosis of anti-Imatinib BaF3 cells expressing Bcr-Abl mutant T315I and E255K. 30 μM AG-490 not only inhibited Epo-induced wild-type JAK2 phosphorylation, but also inhibited constitutive JAK2 V617F mutant phosphorylation. AG-490 acts on BaF3 cells and effectively inhibits cytokine-independent cell growth induced by JAK 2 V617F mutation. |
| in vivo study | AG-490 treatment greatly reduced CD45 in vivo, AG-490 treatment, causing apoptosis of mouse myeloma cells, but did not inhibit IL-12-induced macrophage activation and IFN-γ production. Consistent with inhibiting JAK2 V617F mutation activity in vitro, AG-490 treated nude mice at 0.5 mg per day for 10 days efficiently inhibited JAK2 V617F mutation-induced tumor formation and tumor cell invasion. |
Last Update：2024-04-09 20:52:54
Supplier List
Multiple SpecificationsSpot supply
Product Name: AG-490 (Tyrphostin B42) Visit Supplier Webpage Request for quotationCAS: 133550-30-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Multiple SpecificationsSpot supply
Product Name: AG-490 (Tyrphostin B42) Visit Supplier Webpage Request for quotationCAS: 133550-30-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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